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COX
COX Products
- All (121)
- COX Inhibitors (120)
- COX Modulator (1)
- New COX Products
| Catalog No. | Product Name | Information | Product Use Citations | Product Validations |
|---|---|---|---|---|
| S1261 | Celecoxib | Celecoxib is a selective COX-2 inhibitor with IC50 of 40 nM in Sf9 cells. |
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| S1396 | Resveratrol | Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases（LOX, IC50=2.7 μM）, kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis. |
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| S1204 | Melatonin | Melatonin is a MT receptor agonist, used as a dietary supplement. Melatonin is a selective ATF-6 inhibitor and downregulates COX-2. Melatonin enhances mitophagy and regulates the homeostasis of apoptosis and autophagy. |
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| S4028 | Dexamethasone Sodium Phosphate | Dexamethasone (Dexamethasone 21-phosphate disodium salt) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. |
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| S3017 | Aspirin | Aspirin is a salicylate, and irreversible COX1 and COX2 inhibitor, used as an analgesic to relieve minor aches and pains, as an antipyretic to reduce fever, and as an anti-inflammatory medication. Aspirin induces autophagy and stimulates mitophagy. | ||
| S1576 | Sulfasalazine | Sulfasalazine is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy. | ||
| S1723 | Indomethacin | Indomethacin is a nonselective COX1 and COX2 inhibitor with IC50 of 0.1 μg/mL and 5 μg/mL, respectively, used to reduce fever, pain, stiffness, and swelling. |
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| S8433 | NS-398 (NS398) | NS-398 (N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide) is a selective inhibitor of cyclooxygenase-2 (COX-2). The IC50 values for human recombinant COX-1 and -2 are 75 and 1.77 μM, respectively. |
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| S2007 | Sulindac | Sulindac(MK-231) is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis, used in the treatment of acute or chronic inflammatory conditions. |
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| S2903 | Lumiracoxib | Lumiracoxib (COX-189) is a novel, selective COX-2 inhibitor with Ki of 0.06 μM. It also inhibits COX1 with Ki of 3 μM. |
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| S2410 | Paeoniflorin (NSC 178886) | Paeoniflorin (NSC 178886,Peoniflorin) is a herbal constituent extracted from the root of Paeonia albiflora Pall. Paeoniflorin reduces COX-2 expression. Paeoniflorin alleviates liver fibrosis by inhibiting HIF-1α through mTOR-dependent pathway. | ||
| S7889 | Xanthohumol | Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. Xanthohumol inhibits diacylglycerol acyltransferase 1 (DGAT1) and DGAT2 with both IC50 of 40 μM. Xanthohumol is also a potent antiviral agent against a series of DNA and RNA viruses. Xanthohumol induces growth inhibition and apoptosis in cancer cells. Phase 1. | ||
| S4686 | Vitamin E | Vitamin E (D-alpha-Tocopherol) is a fat-soluble vitamin with potent antioxidant properties. It is a potent peroxyl radical scavenger and inhibits noncompetitively cyclooxygenase activity in many tissues, also inhibits angiogenesis and tumor dormancy through suppressing vascular endothelial growth factor (VEGF) gene transcription. | ||
| S1638 | Ibuprofen (NSC 256857) | Ibuprofen (NSC 256857, Dolgesic) is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50 of 13 μM and 370 μM, respectively. | ||
| S3023 | Bufexamac | Bufexamac(Bufexamic acid) is a COX inhibitor for IFN-α release with EC50 of 8.9 μM. |
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| S1734 | Meloxicam | Meloxicam is a selective COX inhibitor, used to relieve pain and fever effects. |
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| S1903 | Diclofenac Sodium | Diclofenac Sodium (GP 45840) is a non-selective COX inhibitor with IC50 of 0.5 μg/ml and 0.5 μg/ml for COX-1 and -2 in intact cells, respectively, used as a nonsteroidal anti-inflammatory drug (NSAID) to relieve pain and reduce swelling in flammation. | ||
| S4295 | Meclofenamate Sodium | Meclofenamate Sodium(CI 583) is a dual COX-1/COX-2 inhibitor with IC50 of 40 nM and 50 nM, respectively, used in the treatment of joint, muscular pain, arthritis and dysmenorrhea. Meclofenamate Sodium is a non-selective gap-junction blocker and a highly selective inhibitor of fat mass and obesity-associated (FTO) enzyme inhibitor. | ||
| S1960 | Pranoprofen | Pranoprofen (Pyranoprofen,Pranopulin) is a non-steroidal COX inhibitor, used as an anti-inflammatory drug in ophthalmology. | ||
| S1959 | Tolfenamic Acid | Tolfenamic Acid(Clotam) is a COX-2 inhibitor with IC50 of 0.2 μM. | ||
| S4049 | Valdecoxib | Valdecoxib is a potent and selective inhibitor of COX-2 with IC50 of 5 nM. |
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| S2040 | Nimesulide | Nimesulide is a relatively COX-2 selective inhibitor with IC50 of 26 μM. |
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| S9190 | Oroxin B | Oroxin B (Hypocretin-2), one of flavonoids isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent, selectively induces tumor-suppressive ER stress in malignant lymphoma cells and has antioxidant activity. Oroxin B significantly inhibits proliferation and induce apoptosis, which may be strongly associated with the inhibiting COX-2/VEGF and PTEN/PI3K/AKT signaling pathway in SMMC-7721 cells, Oroxin B potentially be used as a novel therapeutic agent for liver cancer.COX-2, VEGF, PI3K, and p-AKT expression levels are downregulated, while PTEN is upregulated after Oroxin B treatment. | ||
| S3931 | Ginsenoside Rd | Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively. | ||
| S5010 | Indometacin Sodium | Indometacin Sodium (Indomethacin Sodium) is the sodium salt of indomethacin, which is a non-selective, reversible, and competitive inhibitor of cyclooxygenases 1 and 2 with anti-inflammatory, analgesic-antipyretic and tocolytic effects. | ||
| S3925 | (-)-Epicatechin gallate | (-)-Epicatechin gallate (ECG) is an inhibitor of cyclooxygenase-1 (COX-1) with IC50 of 7.5 μM. | ||
| S1328 | Etodolac | Etodolac(AY-24236) is a nonsteroidal anti-inflammatory drug (NSAID) and a COX inhibitor, used for the treatment of inflammation and pain. | ||
| S1645 | Ketoprofen | Ketoprofen (RP-19583) is a dual COX1/2 inhibitor, used as a nonsteroidal anti-inflammatory drug to treat arthritis-related inflammatory pains. | ||
| S1646 | Ketorolac | Ketorolac is a non-selective COX inhibitor of COX-1 and COX-2 with IC50 of 1.23 μM and 3.50 μM, respectively. | ||
| S1626 | Naproxen Sodium | Naproxen Sodium (RS-3650) is a COX inhibitor for COX-1 and COX-2 with IC50 of 8.7 μM and 5.2 μM, respectively. | ||
| S5177 | Naproxen | Naproxen is an anti-inflammatory agent with analgesic and antipyretic properties. It is a nonselective inhibitor of COX-1 and COX-2. | ||
| S4078 | Mefenamic Acid | Mefenamic Acid (CI 473, CN-35355) is a competitive inhibitor of COX-1 and COX-2. | ||
| S2351 | Salicin | Salicin (Salicoside, Salicine) is a phenol β-glycosid produced from willow bark that shows anti-inflammatory effects. It is a natural, non-selective COX-1 and COX-2 inhibitor. | ||
| S6686 | SC-560 | SC-560 is a highly selective COX-1 inhibitor with IC50 of 9 nM, compared with the IC50 of 6.3 μM for COX-2, nearly 1,000-fold higher than with COX-1. | ||
| S1255 | Nepafenac | Nepafenac (AHR 9434, AL 6515) is a prodrug of amfenac that acts as an inhibitor of COX-1 and COX-2 activity, used in the treatment of pain and inflammation associated with cataract surgery. | ||
| S3043 | Rofecoxib | Rofecoxib (MK-0966) is a COX-2 inhibitor with IC50 of 18 nM. | ||
| S1713 | Piroxicam | Piroxicam (CP 16171) is a non-selective COX inhibitor, used in the treatment of rheumatoid and osteoarthritis. | ||
| S2577 | Phenacetin | Phenacetin (Acetophenetidin) is a non-opioid analgesic without anti-inflammatory properties. | ||
| S3018 | Niflumic acid | Niflumic acid(Nifluril) is an inhibitor of cyclooxygenase-2 used for joint and muscular pain. | ||
| S2121 | Licofelone (ML3000) | Licofelone (ML3000, Compound 3e) is a dual inhibitor of COX and 5-lipoxygenase (5-LOX) with IC50 of 0.21 μM and 0.18 μM, respectively. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins. Licofelone is considered as a treatment for osteoarthritis. | ||
| S3200 | Triflusal | Triflusal (UR1501) irreversibly inhibits the production of thromboxane-B2 in platelets by acetylating cycloxygenase-1. | ||
| S5698 | Ketorolac tromethamine salt | Ketorolac tromethamine is a synthetic pyrrolizine carboxylic acid derivative with anti-inflammatory, analgesic and antipyretic properties. It is a non-selective COX inhibitor with IC50s of 20 nM for both COX-1 and COX-2. | ||
| S4628 | (+/-)-Sulfinpyrazone | Sulfinpyrazone (G-28315, NSC 75925) is one of the most studied platelet COX inhibitors, also a uricosuric agent that competitively inhibits uric acid reabsorption in kidney proximal tubules. | ||
| S4136 | Carprofen | Carprofen inhibits canine COX2 with IC50 of 30 nM. | ||
| S3168 | cis-Resveratrol | cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively. | ||
| S5640 | Ethyl caffeate | Ethyl caffeate, a naturally occurring compound found in Bidens pilosa, suppresses NF-kappaB activation and its downstream inflammatory mediators, iNOS, COX-2 and PGE2 in vitro. | ||
| S3974 | (+)-Catechin hydrate | (+)-Catechin hydrate is a plant derived polyphenolic anti-oxidants with phytotoxic properties. (+)-Catechin hydrate is a frequent component of traditional herbal remedies, such as Uncaria rhynchophylla. (+)-Catechin hydrate inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM. | ||
| S4656 | Parecoxib | Parecoxib (SC-69124, Valus-P, Vorth-P) is a selective COX2 inhibitor. | ||
| S4651 | Etoricoxib | Etoricoxib (Arcoxia, MK-663, MK-0663, Tauxib, Algix, Nucoxia) is a new COX-2 selective inhibitor with anti-inflammatory, antipyretic, analgesic, and potential antineoplastic properties. | ||
| S2995 | 4-Hydroxyphenylpyruvic acid | 4-Hydroxyphenylpyruvic acid (4-HPPA), an abundant colon metabolite of polyphenols, is a potent scavenger that suppresses levels of free radicals and cyclooxygenase-2 (COX-2) and contributes to reduced risk of colon cancer development. | ||
| S5595 | 3-Carene | 3-Carene (Carene, Delta-3-Carene) is a bicyclic monoterpene in essential oils extracted from pine trees. 3-Carene have potent pharmacological effects on COX-2 overexpression and LPS-induced migration of Raw264.7 macrophages. 3‐carene is shown to significantly stimulate the activity and expression of alkaline phosphatase, an early phase marker of osteoblastic differentiation. | ||
| S2349 | Rutaecarpine | Rutaecarpine (Rutecarpine) is an indolopyridoquinazolinone alkaloid isolated from Evodia rutaecarpa and related herbs; a new class of COX-2 inhibitor. | ||
| S4526 | Fenbufen | Fenbufen (Lederfen, CL-82204) is an orally active phenylalkanoic derivative with anti-inflammatory, analgesic and antipyretic activity. It is a non-steroidal anti-inflammatory drug. | ||
| S9502 | Madecassic acid | Madecassic acid (Brahmic acid), a natural triterpene first isolated from C. asiatica, has diverse anti-inflammatory and anti-diabetic effects, blocking NF-κB activation in macrophages and causing by iNOS, COX-2, TNF-alpha, IL-1beta and IL-6 inhibition. | ||
| S4539 | Salicylic acid | Salicylic acid (2-Hydroxybenzoic acid) is a beta hydroxy acid that occurs as a natural compound in plants which is an inhibitor of ethylene biosynthesis and cyclooxygenase activity. | ||
| S9149 | Benzoylpaeoniflorin | Benzoylpaeoniflorin, a natural product isolated from Chinese paeony root, could inhibit COX-1 and COX-2 in vitro. | ||
| S1761 | Suprofen | Suprofen(TN-762) is a dual COX-1/COX-2 inhibitor, used as a non-steroidal anti-inflammatory analgesic and antipyretic. | ||
| S1518 | Ibuprofen Lysine | Ibuprofen Lysine is a non-steroidal anti-inflammatory drug. | ||
| S2047 | Lornoxicam | Lornoxicam (Chlortenoxicam) is a non-steroidal COX-1/COX-2 inhibitor, used as an anti-inflammatory drug to treat pain, osteoarthritis, and rheumatoid arthritis. | ||
| S2531 | Asaraldehyde | Asaraldehyde (Asaronaldehyde) is a natural COX-2 inhibitor, exhibiting 17-fold selectivity over COX-1. | ||
| S3008 | Zaltoprofen | Zaltoprofen(CN100,Soleton) is an inhibitor of COX-1 and COX-2 for treatment of arthritis. | ||
| S2602 | Acemetacin | Acemetacin (K-708,TVX 1322) is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor. | ||
| S4149 | Amfenac Sodium Monohydrate | Amfenac Sodium monohydrate is a non-steroidal analgesic anti-inflammatory drug with acetic acid moiety. The IC50 values for COX1 and COX2 is 250 nM and 150 nM, respectively. | ||
| S4248 | Bromfenac Sodium | Bromfenac Sodium (AHR 10282R,Bromsite,Bromday,Prolensa,Xibrom) is a nonsteroidal anti-inflammatory drug (NSAID), which has anti-inflammatory activity and may block prostaglandin synthesis by inhibiting cyclooxygenase 1 and 2. | ||
| S4051 | Nabumetone | Nabumetone (BRL-14777) is a non-steroidal anti-inflammatory drug and its active metabolite inhibits the COX. | ||
| S3173 | Antipyrine | Antipyrine (Phenazone,Phenazon) is an analgesic and antipyretic agent; selective COX-3 inhibitor. | ||
| S4011 | Ampiroxicam | Ampiroxicam (CP 65703) is a nonselective cyclooxygenase inhibitor uesd as anti-inflammatory drug. | ||
| S5192 | S-(+)-Ketoprofen | S-(+)-Ketoprofen (Compound 1, Actron, (S)-Ketoprofen, Dexketoprofen) is a potent inhibitor of cyclooxygenase (COX) with IC50 of 1.9 nM and 27 nM for COX-1 and COX-2, respectively. | ||
| S9208 | Ginsenoside Rb3 | Ginsenoside Rb3, extracted from the plant Panax ginseng, plays important roles in cardiovascular diseases, including myocardial ischemia-reperfusion (I/R) injury. Ginsenoside Rb3 (0.1-10 μM) is tested for inhibition of tumor necrosis factor-α (TNF)-induced nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) luciferase reporter activity using a human kidney 293T cell-based assay. Ginsenoside Rb3 shows the significant activity with an IC50 of 8.2 μM. Ginsenoside Rb3 also inhibits the induction of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) messenger Ribonucleic acid (mRNA) in a dose-dependent manner after HepG2 cells have been treated with TNF-α (10 ng/mL). | ||
| S0931 | Jaceosidin | Jaceosidin, a flavonoid isolated from Artemisia vestita, possesses anti-tumor and anti-proliferative activities in many cancer cells. Jaceosidin induces apoptosis, activates Bax and down-regulates Mcl-1 and c-FLIP expression. Jaceosidin inhibits COX-2 expression and NF-κB activation. | ||
| E1949New | DuP-697 | DuP-697 is a potent, irreversible, selective, and orally active inhibitor of COX-2 with an IC50 value of 10 nM for human COX-2, respectively. DuP-697 exerts antiproliferative, antiangiogenic, and apoptotic effects in colorectal cancer cells. | ||
| S5418 | Parecoxib Sodium | Parecoxib Sodium (SC-69124) is a water-soluble, injectable sodium salt form of parecoxib, which is a potent and selective inhibitor of cyclo-oxygenase-2 (COX2). | ||
| S3969 | Veratric acid | Veratric acid (3,4-Dimethoxybenzoic acid), a simple benzoic acid derived from plants and fruits, has anti-oxidant, anti-inflammation, and blood pressure-lowering effects. Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation. | ||
| P1241New | Bromelain | Bromelain is an aqueous extract of pineapple that is composed of 95%-mixture of proteases, acting as an inhibitor of Prostaglandin E2 (PGE2) and Cox-2. It exhibits potent anti-inflammatory, anti-thrombotic, fibrinolytic and anti-cancer functions. | ||
| S9236 | α-Cyperone | α-Cyperone (alpha-cyperone), a major active compound of Cyperus rotundus, exhibits biological activities, such as antivirulence, antigenotoxic, and antibacterial activities. α-Cyperone (alpha-cyperone) is associated with the down-regulation of COX-2, IL-6, Nck-2, Cdc42 and Rac1. | ||
| S3816 | Dehydroevodiamine | Dehydroevodiamine (DHED), a constituent of Evodia rutaecarpa, has various biological effects such as hypotensive, negative chronotropic, ion channel depressant, inhibition of nitric oxide production and cerebral blood flow enhancing activities. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells. | ||
| E0500 | Firocoxib (ML 1785713) | Firocoxib (ML 1785713) is a cyclooxygenase (COX)-2 inhibitor and a nonsteroidal anti-inflammatory drug. In vitro firocoxib inhibits COX-1 and COX-2 with an IC50 of 7.5 mM and 0.13 mM respectively in feline blood. | ||
| S0821 | Pamicogrel | Pamicogrel (KBT3022) is an inhibitor of cyclooxygenase (COX) with platelet anti-aggregatory properties. | ||
| S4032 | Bismuth Subsalicylate | Bismuth Subsalicylate is the active ingredient in Pepto-Bismol and inhibits prostaglandin G/H Synthase 1/2. | ||
| S0759 | FPL 62064 | FPL 62064 is a potent dual inhibitor of 5-lipoxygenase (5-LOX) and prostaglandin synthetase (cyclooxygenase, COX) with IC50 of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and seminal vesicle prostaglandin synthetase, respectively. FPL 62064 has potent anti-inflammatory activity. | ||
| S0761 | Desmethyl Celecoxib | Desmethyl Celecoxib (compound 3b), an analog of Celecoxib with the optimal yield of 75%, is a selective inhibitor of cyclooxygenase-2 (COX-2) with anti-inflammatory activities. | ||
| S0762 | SC 236 | SC-236 is a potent, selective, orally active inhibitor of COX-2 with an IC50 of 10 nM and approximately 18,000-fold COX-2 selectivity. | ||
| S0766 | RHC 80267 | RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL, DAG lipase) with IC50 of 4 μM for cholinesterase activity. RHC 80267 inhibits cyclooxygenase (COX) activity, phospholipase C (PLC) activity and the hydrolysis of phosphatidylcholine (PC). | ||
| S4435 | Metamizole sodium hydrate | Metamizole (Dipyrone) sodium hydrate is a potent inhitior of cyclooxygenase (COX) with strong analgesic as well as antipyretic and spasmolytic properties. | ||
| S3063 | Diclofenac Diethylamine | Diclofenac diethylamine is a nonsteroidal anti-inflammatory drug taken to reduce inflammation and as an analgesic reducing pain in certain conditions. Diclofenac exerts its action via inhibition of prostaglandin synthesis by inhibiting cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) with relative equipotency. | ||
| S6615 | ATB 346 | ATB 346, a novel hydrogen sulphide-releasing derivative of naproxen with remarkably reduced toxicity, inhibits COX activity. ATB 346 is an anti-inflammatory agent that induces apoptosis of human melanoma cells. | ||
| E4987New | (S)-Flurbiprofen | (S)-Flurbiprofen (Esflurbiprofen), an active enantiomer of Flurbiprofen, acts as an inhibitor of cyclooxygenase (COX-2) with an IC50 value of 0.48 μM, respectively. It also helps in the significant reduction of the inflammatory mediator-induced CGRP release. | ||
| S4609 | Diflunisal | Diflunisal (Dolobid, Dolobis, Flovacil, Fluniget,MK-647) is a difluorophenyl derivate of salicylic acid and a nonsteroidal anti-inflammatory drug (NSAID) with antipyretic, analgesic and anti-inflammatory properties. The mechanism of action of diflunisal is as a Cyclooxygenase Inhibitor. | ||
| E4807New | Dexketoprofen trometamol | Dexketoprofen trometamol (Dexketoprofen tromethamine salt) is an orally active non-selective inhibitor of COX. Dexketoprofen trometamol exhibits analgesic efficacy and can be used in treating acute pain. | ||
| S4176 | Trometamol | Trometamol(Tromethamine) is a proton acceptor used to treat acidemia. | ||
| S5520 | Phenidone | Phenidone (1-phenyl-3-pyrazolidinone), a dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), is an organic compound that is primarily used as a photographic developer. | ||
| E0789 | SC-58125 | SC-58125 is a potent and selective inhibitor of human cyclooxygenase 2 (hCOX-2) and triple mutant of hCOX-2, with an IC50 of 0.04 μM and 1 µM, respectively. | ||
| S9029 | Prim-o-glucosylcimifugin | Prim-O-glucosylcimifugin (Cimifugin beta-D-glucopyranoside, Cimifugin 7-glucoside) is a major constituent in Radix Saposhnikovia that has been long used for the treatment of pyrexia, rheumatism, and cancer in traditional Chinese medicine. It shows potential anticancer activity. Prim-O-glucosylcimifugin downregulates the mRNA and protein expression inducible NO synthase (iNOS) and cyclooxygenase 2 (COX-2) in LPS-activated RAW 264.7 macrophages in a concentration-dependent manner. | ||
| S5786 | Bromfenac sodium hydrate | Bromfenac sodium hydrate (Bromsite, Bromday, Prolensa, Xibrom), a brominated nonsteroidal anti-inflammatory drugs (NSAID) with strong in vitro anti-inflammatory potency, is a potent and orally active inhibitor of COX with IC50 of 5.56 nM and 7.45 nM for COX-1 and COX-2, respectively. | ||
| S5019 | Indobufen | Indobufen (Ibustrin, K 3920) is a reversible platelet aggregation inhibitor. Indobufen is a reversible inhibitor of platelet cyclooxygenase (Cox) activity and suppresses thromboxane synthesis. | ||
| S9386 | Polygalacic acid | Polygalacic acid is the triterpenoid tetrahydroxyacid isolated from Polygala paenea L.. Polygalacic acid (0-100 μM; 24 hours) significantly decreases the mRNAexpressions of MMP-3, MMP-9, MMP-13 and COX-2, which are significantly increased by IL-1β, in a dose-dependent manner. | ||
| E3594 | Radix tetrastigme Extract | Radix Tetrastigme Extract is extracted from Tetrastigma hemsleyanum, which can modulate TLR4/COX-2/NF-κB signaling pathway. | ||
| S2595 | FK-3311 | FK-3311 (COX-2 Inhibitor V) is a selective, cell-permeable and orally available inhibitor of cyclooxygenase-2 (COX-2) with antiinflammatory. FK-3311 has protective effects against hepatic warm ischemia-reperfusion injury by marked inhibition of TxA2. | ||
| S6850 | NE 52-QQ57 | NE 52-QQ57 is a selective, and orally available antagonist of G-protein coupled receptor 4 (GPR4) with IC50 of 0.07 μM. NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with NE 52-QQ57 significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2). | ||
| E2274 | Hexahydrocurcumin | Hexahydrocurcumin is one of the major metabolites of curcumin and a selective, orally active COX-2 inhibitor, which has antioxidant, anticancer and anti-inflammatory activities. | ||
| S6073 | Diclofenac acid | Diclofenac acid is a nonsteroidal anti-inflammatory drug that has analgesic, anti-inflammatory, and antipyretic properties, and has been shown to be effective in treating a variety of acute and chronic pain and inflammatory conditions. It inhibits cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) with relative equipotency. | ||
| S4765 | Syringaldehyde | Syringaldehyde (Syringic aldehyde) is an organic compound that occurs naturally in trace amounts. It possesses worthy bioactive properties and is, therefore, used in pharmaceuticals, food, cosmetics, textiles, pulp and paper industries, and even in biological control applications. Syringaldehyde is a polyphenolic compound belonging to the group of flavonoids and is found in different plant species like Manihot esculenta and Magnolia officinalis. Syringaldehyde moderately inhibits COX-2 activity with an IC50 of 3.5 μg/mL[2]. Anti-hyperglycemic and anti-inflammatory activities. | ||
| E4889New | Glafenine | Glafenine (Glafenin) is a non-steroidal anti-inflammatory drug (NSAID) and is a non-narcotic analgesic agent that not only acts as a proteostasis modulator but is also one of the most potent NSAID correctors of F508del-CFTR. It exhibits COX-2 inhibition in the arachidonic acid pathway and rescues class 2 CFTR mutants. | ||
| S4230 | Oxaprozin | Oxaprozin (WY-21743,nsc 310839) is a non-narcotic, non-steroidal anti-inflammatory drug (NSAID) used to relieve the inflammation, swelling, stiffness, and joint pain associated with osteoarthritis and rheumatoid arthritis. | ||
| S2272 | Indoprofen | Indoprofen is a nonsteroidal anti-inflammatory drug (NSAID) and cyclooxygenase (COX) inhibitor. Indoprofen prevents muscle wasting in aged mice through activation of PDK1/AKT pathway.Indoprofen selectively increases SMN2-luciferase reporter protein and endogenous SMN protein. | ||
| S4360 | Tolmetin Sodium | Tolmetin(MCN2559) is a non-steroidal anti-inflammatory drug of the arylalkanoic acids. Tolmetin sodium dihydrate is a non-steroidal antiinflammatory agent, and acts as a non-selective COX inhibitor. | ||
| S3899 | Hederagenin | Hederagenin (Caulosapogenin, Hederagenol, Hederagenic acid, Astrantiagenin E) is a highly water insoluble triterpenoid compound that can be found in various plants including Hedera helix and Chenopodium quinoa. It exhibits a variety of biological activities, including potent antitumor properties both in vitro and in vivo. Hederagenin inhibits LPS-stimulated expression of iNOS, COX-2, and NF-κB. | ||
| S5551 | 6-Paradol | 6-Paradol is a minor constituent of ginger, mainly formed from 6-gingerol via 6-shogaol, and exhibits a variety of biological activities including anti-cancer, anti-inflammatory, and anti-oxidative activities. Paradol is an inhibitor of cyclooxygenase (COX)-2. | ||
| S6457 | Flurbiprofen Axetil | Flurbiprofen Axetil is one of the commonly used nonsteroidal anti-inflammatory drugs (NSAIDs) that nonselectively inhibits cyclooxygenase. | ||
| S6685 | Mavacoxib | Mavacoxib (Trocoxil) is a selective, long-acting cyclooxygenase-2 (COX-2) inhibitor. Mavacoxib is a novel nonsteroidal anti-inflammatory drug (NSAID). | ||
| S4509 | 4-Aminoantipyrine | 4-Aminoantipyrine(Ampyrone) is a metabolite of aminopyrine with analgesic, anti-inflammatory, and antipyretic properties. It is used as a reagent for biochemical reactions producing peroxides or phenols. | ||
| S3261 | Myrislignan | Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan inhibits interleukin-6 (IL-6) and tumour necrosis factor-α (TNF-α). Myrislignan significantly inhibits the expressions of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2) dose-dependently in LPS-stimulated macrophage cells. Myrislignan inhibits the NF-κB signalling pathway activation. | ||
| S3872 | Guaiacol | Guaiacol (O-methoxyphenol, 2-hydroxyanisole, O-methylcatechol) is a phenolic natural product first isolated from Guaiac resin and the oxidation of lignin. It is a precursor to various flavorants, such as eugenoland vanillin. Guaiacol, a phenolic compound isolated from Guaiac resin, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Anti-inflammatory activity. | ||
| S5309 | Propyphenazone (4-Isopropylantipyrine) | Propyphenazone(4-Isopropylantipyrine, Isopropyrine), an analgesic and antipyretic agent, is a selective cyclooxygenase-2 inhibitor with anti-inflammatory activity. | ||
| E0226 | Chebulagic acid | Chebulagic acid, isolated form Terminalia chebula Retz, is a reversible and non-competitive inhibitor of maltase with a Ki value of 6.6 μM. Chebulagic acid shows potent anti-inflammatory effects in LPS-stimulated RAW 264.7 cells. Chebulagic acid also shows potent COX–LOX dual inhibition activity with IC50 values of 15 μM, 0.92 μM and 2.1 μM for COX-1, COX-2 and 5-LOX respectively. |
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| S3304 | Stylopine | Stylopine ((R,S)-Stylopine, Tetrahydrocoptisine) reduces nitric oxide (NO), prostaglandin E2 (PGE2), tumor necrosis factor-alpha (TNF-alpha) and interleukin-1beta (IL-1beta), and the IL-6 production and cyclooxygenase-2 (COX-2) activity caused by the LPS stimulation. Stylopine is a major component of the leaf of Chelidonium majus L. | ||
| S2108 | Flunixin Meglumin | Flunixin Meglumin(Banamine) is a potent inhibitor of the enzyme cyclooxygenase (COX) used as analgesic agent with anti-inflammatory and antipyretic activity. | ||
| S6780 | TFAP | TFAP (N-(5-Aminopyridin-2-yl)-4-(trifluoromethyl)benzamide) is a selective and cell-permeable cyclooxygenase-1 (COX-1) inhibitor with IC50 of 0.8 μM. | ||
| S3255 | Pectolinarigenin | Pectolinarigenin, an active anti-inflammatory ingredient in Cirsium chanroenicum, is a dual inhibitor of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX). | ||
| S5711 | Deracoxib | Deracoxib (SC-046) is a COX-2 inhibitor with >48-fold selectivity over COX-1. It also exhibits inhibitory activity against phosphodiesterase (Ki = 3.6 μM against human PDE4D3). | ||
| S3283 | Marmesin | Marmesin (S-(+)-Marmesin, (+)-Marmesin, (S)-Marmesin) is a natural coumarin with COX-2 and 5-LOX dual inhibitory activity. | ||
| S1261 | Celecoxib | Celecoxib is a selective COX-2 inhibitor with IC50 of 40 nM in Sf9 cells. |
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| S1396 | Resveratrol | Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases（LOX, IC50=2.7 μM）, kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis. |
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| S1204 | Melatonin | Melatonin is a MT receptor agonist, used as a dietary supplement. Melatonin is a selective ATF-6 inhibitor and downregulates COX-2. Melatonin enhances mitophagy and regulates the homeostasis of apoptosis and autophagy. |
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| S4028 | Dexamethasone Sodium Phosphate | Dexamethasone (Dexamethasone 21-phosphate disodium salt) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. |
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| S3017 | Aspirin | Aspirin is a salicylate, and irreversible COX1 and COX2 inhibitor, used as an analgesic to relieve minor aches and pains, as an antipyretic to reduce fever, and as an anti-inflammatory medication. Aspirin induces autophagy and stimulates mitophagy. | ||
| S1576 | Sulfasalazine | Sulfasalazine is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy. | ||
| S1723 | Indomethacin | Indomethacin is a nonselective COX1 and COX2 inhibitor with IC50 of 0.1 μg/mL and 5 μg/mL, respectively, used to reduce fever, pain, stiffness, and swelling. |
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| S8433 | NS-398 (NS398) | NS-398 (N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide) is a selective inhibitor of cyclooxygenase-2 (COX-2). The IC50 values for human recombinant COX-1 and -2 are 75 and 1.77 μM, respectively. |
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| S2007 | Sulindac | Sulindac(MK-231) is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis, used in the treatment of acute or chronic inflammatory conditions. |
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| S2903 | Lumiracoxib | Lumiracoxib (COX-189) is a novel, selective COX-2 inhibitor with Ki of 0.06 μM. It also inhibits COX1 with Ki of 3 μM. |
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| S2410 | Paeoniflorin (NSC 178886) | Paeoniflorin (NSC 178886,Peoniflorin) is a herbal constituent extracted from the root of Paeonia albiflora Pall. Paeoniflorin reduces COX-2 expression. Paeoniflorin alleviates liver fibrosis by inhibiting HIF-1α through mTOR-dependent pathway. | ||
| S7889 | Xanthohumol | Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. Xanthohumol inhibits diacylglycerol acyltransferase 1 (DGAT1) and DGAT2 with both IC50 of 40 μM. Xanthohumol is also a potent antiviral agent against a series of DNA and RNA viruses. Xanthohumol induces growth inhibition and apoptosis in cancer cells. Phase 1. | ||
| S4686 | Vitamin E | Vitamin E (D-alpha-Tocopherol) is a fat-soluble vitamin with potent antioxidant properties. It is a potent peroxyl radical scavenger and inhibits noncompetitively cyclooxygenase activity in many tissues, also inhibits angiogenesis and tumor dormancy through suppressing vascular endothelial growth factor (VEGF) gene transcription. | ||
| S1638 | Ibuprofen (NSC 256857) | Ibuprofen (NSC 256857, Dolgesic) is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50 of 13 μM and 370 μM, respectively. | ||
| S3023 | Bufexamac | Bufexamac(Bufexamic acid) is a COX inhibitor for IFN-α release with EC50 of 8.9 μM. |
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| S1734 | Meloxicam | Meloxicam is a selective COX inhibitor, used to relieve pain and fever effects. |
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| S1903 | Diclofenac Sodium | Diclofenac Sodium (GP 45840) is a non-selective COX inhibitor with IC50 of 0.5 μg/ml and 0.5 μg/ml for COX-1 and -2 in intact cells, respectively, used as a nonsteroidal anti-inflammatory drug (NSAID) to relieve pain and reduce swelling in flammation. | ||
| S4295 | Meclofenamate Sodium | Meclofenamate Sodium(CI 583) is a dual COX-1/COX-2 inhibitor with IC50 of 40 nM and 50 nM, respectively, used in the treatment of joint, muscular pain, arthritis and dysmenorrhea. Meclofenamate Sodium is a non-selective gap-junction blocker and a highly selective inhibitor of fat mass and obesity-associated (FTO) enzyme inhibitor. | ||
| S1960 | Pranoprofen | Pranoprofen (Pyranoprofen,Pranopulin) is a non-steroidal COX inhibitor, used as an anti-inflammatory drug in ophthalmology. | ||
| S1959 | Tolfenamic Acid | Tolfenamic Acid(Clotam) is a COX-2 inhibitor with IC50 of 0.2 μM. | ||
| S4049 | Valdecoxib | Valdecoxib is a potent and selective inhibitor of COX-2 with IC50 of 5 nM. |
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| S2040 | Nimesulide | Nimesulide is a relatively COX-2 selective inhibitor with IC50 of 26 μM. |
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| S9190 | Oroxin B | Oroxin B (Hypocretin-2), one of flavonoids isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent, selectively induces tumor-suppressive ER stress in malignant lymphoma cells and has antioxidant activity. Oroxin B significantly inhibits proliferation and induce apoptosis, which may be strongly associated with the inhibiting COX-2/VEGF and PTEN/PI3K/AKT signaling pathway in SMMC-7721 cells, Oroxin B potentially be used as a novel therapeutic agent for liver cancer.COX-2, VEGF, PI3K, and p-AKT expression levels are downregulated, while PTEN is upregulated after Oroxin B treatment. | ||
| S3931 | Ginsenoside Rd | Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively. | ||
| S5010 | Indometacin Sodium | Indometacin Sodium (Indomethacin Sodium) is the sodium salt of indomethacin, which is a non-selective, reversible, and competitive inhibitor of cyclooxygenases 1 and 2 with anti-inflammatory, analgesic-antipyretic and tocolytic effects. | ||
| S3925 | (-)-Epicatechin gallate | (-)-Epicatechin gallate (ECG) is an inhibitor of cyclooxygenase-1 (COX-1) with IC50 of 7.5 μM. | ||
| S1328 | Etodolac | Etodolac(AY-24236) is a nonsteroidal anti-inflammatory drug (NSAID) and a COX inhibitor, used for the treatment of inflammation and pain. | ||
| S1645 | Ketoprofen | Ketoprofen (RP-19583) is a dual COX1/2 inhibitor, used as a nonsteroidal anti-inflammatory drug to treat arthritis-related inflammatory pains. | ||
| S1646 | Ketorolac | Ketorolac is a non-selective COX inhibitor of COX-1 and COX-2 with IC50 of 1.23 μM and 3.50 μM, respectively. | ||
| S1626 | Naproxen Sodium | Naproxen Sodium (RS-3650) is a COX inhibitor for COX-1 and COX-2 with IC50 of 8.7 μM and 5.2 μM, respectively. | ||
| S5177 | Naproxen | Naproxen is an anti-inflammatory agent with analgesic and antipyretic properties. It is a nonselective inhibitor of COX-1 and COX-2. | ||
| S4078 | Mefenamic Acid | Mefenamic Acid (CI 473, CN-35355) is a competitive inhibitor of COX-1 and COX-2. | ||
| S2351 | Salicin | Salicin (Salicoside, Salicine) is a phenol β-glycosid produced from willow bark that shows anti-inflammatory effects. It is a natural, non-selective COX-1 and COX-2 inhibitor. | ||
| S6686 | SC-560 | SC-560 is a highly selective COX-1 inhibitor with IC50 of 9 nM, compared with the IC50 of 6.3 μM for COX-2, nearly 1,000-fold higher than with COX-1. | ||
| S1255 | Nepafenac | Nepafenac (AHR 9434, AL 6515) is a prodrug of amfenac that acts as an inhibitor of COX-1 and COX-2 activity, used in the treatment of pain and inflammation associated with cataract surgery. | ||
| S3043 | Rofecoxib | Rofecoxib (MK-0966) is a COX-2 inhibitor with IC50 of 18 nM. | ||
| S1713 | Piroxicam | Piroxicam (CP 16171) is a non-selective COX inhibitor, used in the treatment of rheumatoid and osteoarthritis. | ||
| S2577 | Phenacetin | Phenacetin (Acetophenetidin) is a non-opioid analgesic without anti-inflammatory properties. | ||
| S3018 | Niflumic acid | Niflumic acid(Nifluril) is an inhibitor of cyclooxygenase-2 used for joint and muscular pain. | ||
| S2121 | Licofelone (ML3000) | Licofelone (ML3000, Compound 3e) is a dual inhibitor of COX and 5-lipoxygenase (5-LOX) with IC50 of 0.21 μM and 0.18 μM, respectively. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins. Licofelone is considered as a treatment for osteoarthritis. | ||
| S3200 | Triflusal | Triflusal (UR1501) irreversibly inhibits the production of thromboxane-B2 in platelets by acetylating cycloxygenase-1. | ||
| S5698 | Ketorolac tromethamine salt | Ketorolac tromethamine is a synthetic pyrrolizine carboxylic acid derivative with anti-inflammatory, analgesic and antipyretic properties. It is a non-selective COX inhibitor with IC50s of 20 nM for both COX-1 and COX-2. | ||
| S4628 | (+/-)-Sulfinpyrazone | Sulfinpyrazone (G-28315, NSC 75925) is one of the most studied platelet COX inhibitors, also a uricosuric agent that competitively inhibits uric acid reabsorption in kidney proximal tubules. | ||
| S4136 | Carprofen | Carprofen inhibits canine COX2 with IC50 of 30 nM. | ||
| S3168 | cis-Resveratrol | cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively. | ||
| S5640 | Ethyl caffeate | Ethyl caffeate, a naturally occurring compound found in Bidens pilosa, suppresses NF-kappaB activation and its downstream inflammatory mediators, iNOS, COX-2 and PGE2 in vitro. | ||
| S3974 | (+)-Catechin hydrate | (+)-Catechin hydrate is a plant derived polyphenolic anti-oxidants with phytotoxic properties. (+)-Catechin hydrate is a frequent component of traditional herbal remedies, such as Uncaria rhynchophylla. (+)-Catechin hydrate inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM. | ||
| S4656 | Parecoxib | Parecoxib (SC-69124, Valus-P, Vorth-P) is a selective COX2 inhibitor. | ||
| S4651 | Etoricoxib | Etoricoxib (Arcoxia, MK-663, MK-0663, Tauxib, Algix, Nucoxia) is a new COX-2 selective inhibitor with anti-inflammatory, antipyretic, analgesic, and potential antineoplastic properties. | ||
| S2995 | 4-Hydroxyphenylpyruvic acid | 4-Hydroxyphenylpyruvic acid (4-HPPA), an abundant colon metabolite of polyphenols, is a potent scavenger that suppresses levels of free radicals and cyclooxygenase-2 (COX-2) and contributes to reduced risk of colon cancer development. | ||
| S5595 | 3-Carene | 3-Carene (Carene, Delta-3-Carene) is a bicyclic monoterpene in essential oils extracted from pine trees. 3-Carene have potent pharmacological effects on COX-2 overexpression and LPS-induced migration of Raw264.7 macrophages. 3‐carene is shown to significantly stimulate the activity and expression of alkaline phosphatase, an early phase marker of osteoblastic differentiation. | ||
| S2349 | Rutaecarpine | Rutaecarpine (Rutecarpine) is an indolopyridoquinazolinone alkaloid isolated from Evodia rutaecarpa and related herbs; a new class of COX-2 inhibitor. | ||
| S4526 | Fenbufen | Fenbufen (Lederfen, CL-82204) is an orally active phenylalkanoic derivative with anti-inflammatory, analgesic and antipyretic activity. It is a non-steroidal anti-inflammatory drug. | ||
| S9502 | Madecassic acid | Madecassic acid (Brahmic acid), a natural triterpene first isolated from C. asiatica, has diverse anti-inflammatory and anti-diabetic effects, blocking NF-κB activation in macrophages and causing by iNOS, COX-2, TNF-alpha, IL-1beta and IL-6 inhibition. | ||
| S4539 | Salicylic acid | Salicylic acid (2-Hydroxybenzoic acid) is a beta hydroxy acid that occurs as a natural compound in plants which is an inhibitor of ethylene biosynthesis and cyclooxygenase activity. | ||
| S9149 | Benzoylpaeoniflorin | Benzoylpaeoniflorin, a natural product isolated from Chinese paeony root, could inhibit COX-1 and COX-2 in vitro. | ||
| S1761 | Suprofen | Suprofen(TN-762) is a dual COX-1/COX-2 inhibitor, used as a non-steroidal anti-inflammatory analgesic and antipyretic. | ||
| S1518 | Ibuprofen Lysine | Ibuprofen Lysine is a non-steroidal anti-inflammatory drug. | ||
| S2047 | Lornoxicam | Lornoxicam (Chlortenoxicam) is a non-steroidal COX-1/COX-2 inhibitor, used as an anti-inflammatory drug to treat pain, osteoarthritis, and rheumatoid arthritis. | ||
| S2531 | Asaraldehyde | Asaraldehyde (Asaronaldehyde) is a natural COX-2 inhibitor, exhibiting 17-fold selectivity over COX-1. | ||
| S3008 | Zaltoprofen | Zaltoprofen(CN100,Soleton) is an inhibitor of COX-1 and COX-2 for treatment of arthritis. | ||
| S2602 | Acemetacin | Acemetacin (K-708,TVX 1322) is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor. | ||
| S4149 | Amfenac Sodium Monohydrate | Amfenac Sodium monohydrate is a non-steroidal analgesic anti-inflammatory drug with acetic acid moiety. The IC50 values for COX1 and COX2 is 250 nM and 150 nM, respectively. | ||
| S4248 | Bromfenac Sodium | Bromfenac Sodium (AHR 10282R,Bromsite,Bromday,Prolensa,Xibrom) is a nonsteroidal anti-inflammatory drug (NSAID), which has anti-inflammatory activity and may block prostaglandin synthesis by inhibiting cyclooxygenase 1 and 2. | ||
| S4051 | Nabumetone | Nabumetone (BRL-14777) is a non-steroidal anti-inflammatory drug and its active metabolite inhibits the COX. | ||
| S3173 | Antipyrine | Antipyrine (Phenazone,Phenazon) is an analgesic and antipyretic agent; selective COX-3 inhibitor. | ||
| S4011 | Ampiroxicam | Ampiroxicam (CP 65703) is a nonselective cyclooxygenase inhibitor uesd as anti-inflammatory drug. | ||
| S5192 | S-(+)-Ketoprofen | S-(+)-Ketoprofen (Compound 1, Actron, (S)-Ketoprofen, Dexketoprofen) is a potent inhibitor of cyclooxygenase (COX) with IC50 of 1.9 nM and 27 nM for COX-1 and COX-2, respectively. | ||
| S9208 | Ginsenoside Rb3 | Ginsenoside Rb3, extracted from the plant Panax ginseng, plays important roles in cardiovascular diseases, including myocardial ischemia-reperfusion (I/R) injury. Ginsenoside Rb3 (0.1-10 μM) is tested for inhibition of tumor necrosis factor-α (TNF)-induced nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) luciferase reporter activity using a human kidney 293T cell-based assay. Ginsenoside Rb3 shows the significant activity with an IC50 of 8.2 μM. Ginsenoside Rb3 also inhibits the induction of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) messenger Ribonucleic acid (mRNA) in a dose-dependent manner after HepG2 cells have been treated with TNF-α (10 ng/mL). | ||
| S0931 | Jaceosidin | Jaceosidin, a flavonoid isolated from Artemisia vestita, possesses anti-tumor and anti-proliferative activities in many cancer cells. Jaceosidin induces apoptosis, activates Bax and down-regulates Mcl-1 and c-FLIP expression. Jaceosidin inhibits COX-2 expression and NF-κB activation. | ||
| E1949New | DuP-697 | DuP-697 is a potent, irreversible, selective, and orally active inhibitor of COX-2 with an IC50 value of 10 nM for human COX-2, respectively. DuP-697 exerts antiproliferative, antiangiogenic, and apoptotic effects in colorectal cancer cells. | ||
| S5418 | Parecoxib Sodium | Parecoxib Sodium (SC-69124) is a water-soluble, injectable sodium salt form of parecoxib, which is a potent and selective inhibitor of cyclo-oxygenase-2 (COX2). | ||
| S3969 | Veratric acid | Veratric acid (3,4-Dimethoxybenzoic acid), a simple benzoic acid derived from plants and fruits, has anti-oxidant, anti-inflammation, and blood pressure-lowering effects. Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation. | ||
| P1241New | Bromelain | Bromelain is an aqueous extract of pineapple that is composed of 95%-mixture of proteases, acting as an inhibitor of Prostaglandin E2 (PGE2) and Cox-2. It exhibits potent anti-inflammatory, anti-thrombotic, fibrinolytic and anti-cancer functions. | ||
| S9236 | α-Cyperone | α-Cyperone (alpha-cyperone), a major active compound of Cyperus rotundus, exhibits biological activities, such as antivirulence, antigenotoxic, and antibacterial activities. α-Cyperone (alpha-cyperone) is associated with the down-regulation of COX-2, IL-6, Nck-2, Cdc42 and Rac1. | ||
| S3816 | Dehydroevodiamine | Dehydroevodiamine (DHED), a constituent of Evodia rutaecarpa, has various biological effects such as hypotensive, negative chronotropic, ion channel depressant, inhibition of nitric oxide production and cerebral blood flow enhancing activities. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells. | ||
| E0500 | Firocoxib (ML 1785713) | Firocoxib (ML 1785713) is a cyclooxygenase (COX)-2 inhibitor and a nonsteroidal anti-inflammatory drug. In vitro firocoxib inhibits COX-1 and COX-2 with an IC50 of 7.5 mM and 0.13 mM respectively in feline blood. | ||
| S0821 | Pamicogrel | Pamicogrel (KBT3022) is an inhibitor of cyclooxygenase (COX) with platelet anti-aggregatory properties. | ||
| S4032 | Bismuth Subsalicylate | Bismuth Subsalicylate is the active ingredient in Pepto-Bismol and inhibits prostaglandin G/H Synthase 1/2. | ||
| S0759 | FPL 62064 | FPL 62064 is a potent dual inhibitor of 5-lipoxygenase (5-LOX) and prostaglandin synthetase (cyclooxygenase, COX) with IC50 of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and seminal vesicle prostaglandin synthetase, respectively. FPL 62064 has potent anti-inflammatory activity. | ||
| S0761 | Desmethyl Celecoxib | Desmethyl Celecoxib (compound 3b), an analog of Celecoxib with the optimal yield of 75%, is a selective inhibitor of cyclooxygenase-2 (COX-2) with anti-inflammatory activities. | ||
| S0762 | SC 236 | SC-236 is a potent, selective, orally active inhibitor of COX-2 with an IC50 of 10 nM and approximately 18,000-fold COX-2 selectivity. | ||
| S0766 | RHC 80267 | RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL, DAG lipase) with IC50 of 4 μM for cholinesterase activity. RHC 80267 inhibits cyclooxygenase (COX) activity, phospholipase C (PLC) activity and the hydrolysis of phosphatidylcholine (PC). | ||
| S4435 | Metamizole sodium hydrate | Metamizole (Dipyrone) sodium hydrate is a potent inhitior of cyclooxygenase (COX) with strong analgesic as well as antipyretic and spasmolytic properties. | ||
| S3063 | Diclofenac Diethylamine | Diclofenac diethylamine is a nonsteroidal anti-inflammatory drug taken to reduce inflammation and as an analgesic reducing pain in certain conditions. Diclofenac exerts its action via inhibition of prostaglandin synthesis by inhibiting cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) with relative equipotency. | ||
| S6615 | ATB 346 | ATB 346, a novel hydrogen sulphide-releasing derivative of naproxen with remarkably reduced toxicity, inhibits COX activity. ATB 346 is an anti-inflammatory agent that induces apoptosis of human melanoma cells. | ||
| E4987New | (S)-Flurbiprofen | (S)-Flurbiprofen (Esflurbiprofen), an active enantiomer of Flurbiprofen, acts as an inhibitor of cyclooxygenase (COX-2) with an IC50 value of 0.48 μM, respectively. It also helps in the significant reduction of the inflammatory mediator-induced CGRP release. | ||
| S4609 | Diflunisal | Diflunisal (Dolobid, Dolobis, Flovacil, Fluniget,MK-647) is a difluorophenyl derivate of salicylic acid and a nonsteroidal anti-inflammatory drug (NSAID) with antipyretic, analgesic and anti-inflammatory properties. The mechanism of action of diflunisal is as a Cyclooxygenase Inhibitor. | ||
| E4807New | Dexketoprofen trometamol | Dexketoprofen trometamol (Dexketoprofen tromethamine salt) is an orally active non-selective inhibitor of COX. Dexketoprofen trometamol exhibits analgesic efficacy and can be used in treating acute pain. | ||
| S4176 | Trometamol | Trometamol(Tromethamine) is a proton acceptor used to treat acidemia. | ||
| S5520 | Phenidone | Phenidone (1-phenyl-3-pyrazolidinone), a dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), is an organic compound that is primarily used as a photographic developer. | ||
| E0789 | SC-58125 | SC-58125 is a potent and selective inhibitor of human cyclooxygenase 2 (hCOX-2) and triple mutant of hCOX-2, with an IC50 of 0.04 μM and 1 µM, respectively. | ||
| S9029 | Prim-o-glucosylcimifugin | Prim-O-glucosylcimifugin (Cimifugin beta-D-glucopyranoside, Cimifugin 7-glucoside) is a major constituent in Radix Saposhnikovia that has been long used for the treatment of pyrexia, rheumatism, and cancer in traditional Chinese medicine. It shows potential anticancer activity. Prim-O-glucosylcimifugin downregulates the mRNA and protein expression inducible NO synthase (iNOS) and cyclooxygenase 2 (COX-2) in LPS-activated RAW 264.7 macrophages in a concentration-dependent manner. | ||
| S5786 | Bromfenac sodium hydrate | Bromfenac sodium hydrate (Bromsite, Bromday, Prolensa, Xibrom), a brominated nonsteroidal anti-inflammatory drugs (NSAID) with strong in vitro anti-inflammatory potency, is a potent and orally active inhibitor of COX with IC50 of 5.56 nM and 7.45 nM for COX-1 and COX-2, respectively. | ||
| S5019 | Indobufen | Indobufen (Ibustrin, K 3920) is a reversible platelet aggregation inhibitor. Indobufen is a reversible inhibitor of platelet cyclooxygenase (Cox) activity and suppresses thromboxane synthesis. | ||
| S9386 | Polygalacic acid | Polygalacic acid is the triterpenoid tetrahydroxyacid isolated from Polygala paenea L.. Polygalacic acid (0-100 μM; 24 hours) significantly decreases the mRNAexpressions of MMP-3, MMP-9, MMP-13 and COX-2, which are significantly increased by IL-1β, in a dose-dependent manner. | ||
| S2595 | FK-3311 | FK-3311 (COX-2 Inhibitor V) is a selective, cell-permeable and orally available inhibitor of cyclooxygenase-2 (COX-2) with antiinflammatory. FK-3311 has protective effects against hepatic warm ischemia-reperfusion injury by marked inhibition of TxA2. | ||
| S6850 | NE 52-QQ57 | NE 52-QQ57 is a selective, and orally available antagonist of G-protein coupled receptor 4 (GPR4) with IC50 of 0.07 μM. NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with NE 52-QQ57 significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2). | ||
| E2274 | Hexahydrocurcumin | Hexahydrocurcumin is one of the major metabolites of curcumin and a selective, orally active COX-2 inhibitor, which has antioxidant, anticancer and anti-inflammatory activities. | ||
| S6073 | Diclofenac acid | Diclofenac acid is a nonsteroidal anti-inflammatory drug that has analgesic, anti-inflammatory, and antipyretic properties, and has been shown to be effective in treating a variety of acute and chronic pain and inflammatory conditions. It inhibits cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) with relative equipotency. | ||
| S4765 | Syringaldehyde | Syringaldehyde (Syringic aldehyde) is an organic compound that occurs naturally in trace amounts. It possesses worthy bioactive properties and is, therefore, used in pharmaceuticals, food, cosmetics, textiles, pulp and paper industries, and even in biological control applications. Syringaldehyde is a polyphenolic compound belonging to the group of flavonoids and is found in different plant species like Manihot esculenta and Magnolia officinalis. Syringaldehyde moderately inhibits COX-2 activity with an IC50 of 3.5 μg/mL[2]. Anti-hyperglycemic and anti-inflammatory activities. | ||
| E4889New | Glafenine | Glafenine (Glafenin) is a non-steroidal anti-inflammatory drug (NSAID) and is a non-narcotic analgesic agent that not only acts as a proteostasis modulator but is also one of the most potent NSAID correctors of F508del-CFTR. It exhibits COX-2 inhibition in the arachidonic acid pathway and rescues class 2 CFTR mutants. | ||
| S4230 | Oxaprozin | Oxaprozin (WY-21743,nsc 310839) is a non-narcotic, non-steroidal anti-inflammatory drug (NSAID) used to relieve the inflammation, swelling, stiffness, and joint pain associated with osteoarthritis and rheumatoid arthritis. | ||
| S2272 | Indoprofen | Indoprofen is a nonsteroidal anti-inflammatory drug (NSAID) and cyclooxygenase (COX) inhibitor. Indoprofen prevents muscle wasting in aged mice through activation of PDK1/AKT pathway.Indoprofen selectively increases SMN2-luciferase reporter protein and endogenous SMN protein. | ||
| S4360 | Tolmetin Sodium | Tolmetin(MCN2559) is a non-steroidal anti-inflammatory drug of the arylalkanoic acids. Tolmetin sodium dihydrate is a non-steroidal antiinflammatory agent, and acts as a non-selective COX inhibitor. | ||
| S3899 | Hederagenin | Hederagenin (Caulosapogenin, Hederagenol, Hederagenic acid, Astrantiagenin E) is a highly water insoluble triterpenoid compound that can be found in various plants including Hedera helix and Chenopodium quinoa. It exhibits a variety of biological activities, including potent antitumor properties both in vitro and in vivo. Hederagenin inhibits LPS-stimulated expression of iNOS, COX-2, and NF-κB. | ||
| S5551 | 6-Paradol | 6-Paradol is a minor constituent of ginger, mainly formed from 6-gingerol via 6-shogaol, and exhibits a variety of biological activities including anti-cancer, anti-inflammatory, and anti-oxidative activities. Paradol is an inhibitor of cyclooxygenase (COX)-2. | ||
| S6457 | Flurbiprofen Axetil | Flurbiprofen Axetil is one of the commonly used nonsteroidal anti-inflammatory drugs (NSAIDs) that nonselectively inhibits cyclooxygenase. | ||
| S6685 | Mavacoxib | Mavacoxib (Trocoxil) is a selective, long-acting cyclooxygenase-2 (COX-2) inhibitor. Mavacoxib is a novel nonsteroidal anti-inflammatory drug (NSAID). | ||
| S4509 | 4-Aminoantipyrine | 4-Aminoantipyrine(Ampyrone) is a metabolite of aminopyrine with analgesic, anti-inflammatory, and antipyretic properties. It is used as a reagent for biochemical reactions producing peroxides or phenols. | ||
| S3261 | Myrislignan | Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan inhibits interleukin-6 (IL-6) and tumour necrosis factor-α (TNF-α). Myrislignan significantly inhibits the expressions of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2) dose-dependently in LPS-stimulated macrophage cells. Myrislignan inhibits the NF-κB signalling pathway activation. | ||
| S3872 | Guaiacol | Guaiacol (O-methoxyphenol, 2-hydroxyanisole, O-methylcatechol) is a phenolic natural product first isolated from Guaiac resin and the oxidation of lignin. It is a precursor to various flavorants, such as eugenoland vanillin. Guaiacol, a phenolic compound isolated from Guaiac resin, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Anti-inflammatory activity. | ||
| S5309 | Propyphenazone (4-Isopropylantipyrine) | Propyphenazone(4-Isopropylantipyrine, Isopropyrine), an analgesic and antipyretic agent, is a selective cyclooxygenase-2 inhibitor with anti-inflammatory activity. | ||
| E0226 | Chebulagic acid | Chebulagic acid, isolated form Terminalia chebula Retz, is a reversible and non-competitive inhibitor of maltase with a Ki value of 6.6 μM. Chebulagic acid shows potent anti-inflammatory effects in LPS-stimulated RAW 264.7 cells. Chebulagic acid also shows potent COX–LOX dual inhibition activity with IC50 values of 15 μM, 0.92 μM and 2.1 μM for COX-1, COX-2 and 5-LOX respectively. |
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| S3304 | Stylopine | Stylopine ((R,S)-Stylopine, Tetrahydrocoptisine) reduces nitric oxide (NO), prostaglandin E2 (PGE2), tumor necrosis factor-alpha (TNF-alpha) and interleukin-1beta (IL-1beta), and the IL-6 production and cyclooxygenase-2 (COX-2) activity caused by the LPS stimulation. Stylopine is a major component of the leaf of Chelidonium majus L. | ||
| S2108 | Flunixin Meglumin | Flunixin Meglumin(Banamine) is a potent inhibitor of the enzyme cyclooxygenase (COX) used as analgesic agent with anti-inflammatory and antipyretic activity. | ||
| S6780 | TFAP | TFAP (N-(5-Aminopyridin-2-yl)-4-(trifluoromethyl)benzamide) is a selective and cell-permeable cyclooxygenase-1 (COX-1) inhibitor with IC50 of 0.8 μM. | ||
| S3255 | Pectolinarigenin | Pectolinarigenin, an active anti-inflammatory ingredient in Cirsium chanroenicum, is a dual inhibitor of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX). | ||
| S5711 | Deracoxib | Deracoxib (SC-046) is a COX-2 inhibitor with >48-fold selectivity over COX-1. It also exhibits inhibitory activity against phosphodiesterase (Ki = 3.6 μM against human PDE4D3). | ||
| S3283 | Marmesin | Marmesin (S-(+)-Marmesin, (+)-Marmesin, (S)-Marmesin) is a natural coumarin with COX-2 and 5-LOX dual inhibitory activity. | ||
| E3594 | Radix tetrastigme Extract | Radix Tetrastigme Extract is extracted from Tetrastigma hemsleyanum, which can modulate TLR4/COX-2/NF-κB signaling pathway. | ||
| E1949New | DuP-697 | DuP-697 is a potent, irreversible, selective, and orally active inhibitor of COX-2 with an IC50 value of 10 nM for human COX-2, respectively. DuP-697 exerts antiproliferative, antiangiogenic, and apoptotic effects in colorectal cancer cells. | ||
| P1241New | Bromelain | Bromelain is an aqueous extract of pineapple that is composed of 95%-mixture of proteases, acting as an inhibitor of Prostaglandin E2 (PGE2) and Cox-2. It exhibits potent anti-inflammatory, anti-thrombotic, fibrinolytic and anti-cancer functions. | ||
| E4987New | (S)-Flurbiprofen | (S)-Flurbiprofen (Esflurbiprofen), an active enantiomer of Flurbiprofen, acts as an inhibitor of cyclooxygenase (COX-2) with an IC50 value of 0.48 μM, respectively. It also helps in the significant reduction of the inflammatory mediator-induced CGRP release. | ||
| E4807New | Dexketoprofen trometamol | Dexketoprofen trometamol (Dexketoprofen tromethamine salt) is an orally active non-selective inhibitor of COX. Dexketoprofen trometamol exhibits analgesic efficacy and can be used in treating acute pain. | ||
| E4889New | Glafenine | Glafenine (Glafenin) is a non-steroidal anti-inflammatory drug (NSAID) and is a non-narcotic analgesic agent that not only acts as a proteostasis modulator but is also one of the most potent NSAID correctors of F508del-CFTR. It exhibits COX-2 inhibition in the arachidonic acid pathway and rescues class 2 CFTR mutants. |
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