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PPAR

Isoform-selective Products

PPARα PPARβ/δ PPARγ PPARδ

Signaling Pathway

PPAR Products

All (59)
PPAR Inhibitors (9)
PPAR Activators (13)
PPAR Antagonists (5)
PPAR Agonists (28)
PPAR Modulators (4)
New PPAR Products

Catalog No.	Product Name	Information	Product Use Citations
S2871	T0070907	T0070907 is a potent inhibitor of PPARγ (peroxisome proliferator activator receptor γ ) that induces G2/M arrest and enhances the effect of radiation in human cervical cancer cells through mitotic catastrophe. It also acts as an antagonist of PPARγ that suppresses breast cancer cell proliferation and motility via both PPARgamma-dependent and -independent mechanisms.	Immunity, 2024, 57(10):2344-2361.e7 Nat Commun, 2024, 15(1):1429 Bone Res, 2024, 12(1):15
S2556	Rosiglitazone	Rosiglitazone is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action. Rosiglitazone modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.	Nat Commun, 2024, 15(1):1429 Nat Commun, 2024, 15(1):7991 Research (Wash D C), 2024, 7:0400
S2915	GW9662	GW9662 is a selective PPAR antagonist for PPARγ with IC50 of 3.3 nM in a cell-free assay, with at least 10- to 600-fold functional selectivity in cells with PPARγ versus PPARα and PPARδ.	J Hematol Oncol, 2024, 17(1):9 Research (Wash D C), 2024, 7:0400 Int J Biol Sci, 2024, 20(6):2323-2338
S2590	Pioglitazone	Pioglitazone is a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist, used to treat diabetes; A weak activator for full-length hPPARα, but not full-length hPPARδ.	Signal Transduct Target Ther, 2024, 9(1):257 Cell Commun Signal, 2024, 22(1):266 Braz J Med Biol Res, 2024, 57:e13235
S2505	Rosiglitazone maleate	Rosiglitazone maleate, a member of the thiazolidinedione class of antihyperglycaemic agents, is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ (PPAR-γ) with IC50 of 42 nM. Rosiglitazone maleate also modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.	Stem Cell Reports, 2022, 17(11):2531-2547 Cell Death Dis, 2021, 12(11):972 Antioxidants (Basel), 2021, 10(2)155
S7484	FH535	FH535 is a Wnt/β-catenin signaling inhibitor and also a dual PPARγ and PPARδ antagonist.	Int J Biol Sci, 2024, 20(6):2323-2338 Gastroenterology, 2023, S0016-5085(23)00114-2 Gastroenterology, 2023, 164(6):990-1005
S2075	Rosiglitazone HCl	Rosiglitazone HCl is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.	J Immunother Cancer, 2024, 12(11)e009805 Stem Cell Reports, 2022, 17(11):2531-2547 Cell Death Dis, 2021, 12(11):972
S8029	WY-14643 (Pirinixic Acid)	WY-14643 (Pirinixic Acid, NSC 310038) is a potent and selective PPARα activator with an EC50 of 1.5 μM.	Front Pharmacol, 2024, 15:1366479 Front Pharmacol, 2024, 15:1366479 Cell Mol Gastroenterol Hepatol, 2022, 14(6):1311-1331
S2798	GW6471	GW 6471 is a potent antagonist of PPARα with IC50 of 0.24 μM.	Nat Commun, 2024, 15(1):7611 Cancer Lett, 2024, 587:216724 JCI Insight, 2024, 9(6)e171961
S1794	Fenofibrate	Fenofibrate is a compound of the fibrate class and fibric acid derivative. Fenofibrate is a selective agonist of PPARα with EC50 of 30 μM. Fenofibrate binds to and inhibits cytochrome P450 epoxygenase (CYP)2C with IC50 of 0.2 μM, 0.7 μM and 9.7 μM for CYP2C19, CYP2B6 and CYP2C9, respectively. Fenofibrate induces autophagy.	J Immunother Cancer, 2024, 12(11)e009805 Heliyon, 2024, 10(11):e31861 Cancer Lett, 2023, 10.1016/j.canlet.2023.216427
S8025	GSK3787	GSK3787 is a selective and irreversible antagonist of PPARδ with pIC50 of 6.6, with no measurable affinity for hPPARα or hPPARγ.	Drug Des Devel Ther, 2024, 18:4799-4824 Cell Discov, 2023, 9(1):54 Cell Discov, 2023, 9(1):54
S2046	Pioglitazone HCl	Pioglitazone HCl (AD-4833, U-72107E) is an inhibitor of cytochrome P450 (CYP)2C8 and CYP3A4 enzymes. Pioglitazone HCl inhibits CYP2C8, CYP3A4 and CYP2C9 with Ki of 1.7 μM, 11.8 μM and 32.1 μM, respectively. Pioglitazone HCl is also a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist with EC50 of 0.93 μM and 0.99 μM for human PPARγ and mouse PPARγ, respectively. Pioglitazone HCl inhibits mitochondrial iron uptake, lipid peroxidation, and subsequent ferroptosis.	J Transl Med, 2024, 22(1):593 Commun Biol, 2022, 5(1):231 J Genet Genomics, 2022, S1673-8527(22)00133-3
S8020	GW0742	GW0742 is a potent and highly selective PPARβ/δ agonist, with IC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ.	Cell Commun Signal, 2024, 22(1):266 Med Oncol, 2024, 41(8):188 Life Sci, 2021, 279:119696
S7955	EPI-001	EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.	Int J Biol Macromol, 2024, 278(Pt 3):134844 Nat Struct Mol Biol, 2023, 30(12):1958-1969 Int J Mol Sci, 2023, 24(4)3823
S7767	AZ6102	AZ6102 is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows IC50 of 5 nM for Wnt pathway inhibition in DLD-1 cells.	Nat Commun, 2022, 13(1):2070 Sci Adv, 2022, 8(19):eabh2332 Haematologica, 2021, 10.3324/haematol.2020.267096
S3834	Astaxanthin	Astaxanthin (β-Carotene-4,4'-dione, Trans-Astaxanthin), a xanthophyll carotenoid, is a nutrient with unique cell membrane actions and diverse clinical benefits with excellent safety and tolerability. Astaxanthin, a red dietary carotenoid isolated from Haematococcus pluvialis, is a modulator of PPARγ and a potent antioxidant with antiproliferative, neuroprotective and anti-inflammatory activity.	Int Immunopharmacol, 2023, 119:110159 J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493 Aging (Albany NY), 2019, 11(22):10513-10531
S3846	Eupatilin	Eupatilin (NSC 122413), a major flavonoid from Artemisia plants, possesses various beneficial biological effects including anti-inflammation, anti-tumor, anti-cancer, anti-allergy, and anti-oxidation activity. Eupatilin, a lipophilic flavonoid isolated from Artemisia species, is a PPARα agonist, and possesses anti-apoptotic, anti-oxidative and anti-inflammatory activities.	Int J Mol Sci, 2023, 24(6)5933 Front Pharmacol, 2022, 13:940475 Int J Mol Sci, 2022, 23(24)16055
S8432	Troglitazone	Troglitazone is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR) that is a ligand activated transcription factor regulating cell differentiation and growth. Troglitazone induces autophagy, apoptosis and necroptosis in bladder cancer cells. Troglitazone prevents RSL3-induced ferroptosis and lipid peroxidation in Pfa1 cells.	CNS Neurosci Ther, 2024, 30(8):e14911 Int J Mol Med, 2024, 53(4)37 Free Radic Biol Med, 2021, 163:234-242
S5817	GSK0660	GSK0660 is a potent PPARβ/δ antagonist with a pIC50 of 6.8 (binding assay IC50 = 155 nM; antagonist assay IC50 = 300 nM) and is nearly inactive on PPARα and PPARγ with IC50s above approximately 10 μM.	Cells, 2024, 13(3):206. Cells, 2024, 13(3)206 Elife, 2023, 12e82970
S4159	Bezafibrate	Bezafibrate (BM 15075) is the first clinically tested dual and pan-PPAR co-agonism.	Nat Commun, 2021, 12(1):1929 PPAR Res, 2021, 2021:5589342
S9189	Oroxin A	Oroxin A (Baicalein 7-O-glucoside), an active component isolated from the herb Oroxylum indicum (L.) Kurz, activates PPARγ and inhibits α-glucosidase, exerting antioxidant activity.	Front Pharmacol, 2022, 13:894899 An Acad Bras Cienc, 2022, 94(suppl 4):e20211400
S9723	CDDO-Im (RTA-403)	CDDO-Im (RTA-403) is an activator of nuclear factor erythroid 2–related factor 2 (Nrf2) and peroxisome proliferator-activated receptor (PPAR). CDDO-Im binds to PPARα and PPARγ with Ki of 232 nM and 344 nM, respectively. CDDO-Im inhibits inflammatory response and tumor growth in vivo.	Ecotoxicol Environ Saf, 2022, 241:113754 Int J Mol Sci, 2022, 23(19)11715
S4527	Fenofibric acid	Fenofibric acid (NSC 281318, Trilipix, FNF acid) is a fibrate that acts as a lipid-lowering agent, decreasing low-density lipoprotein cholesterol and triglycerides.	J Immunother Cancer, 2024, 12(11)e009805 Front Med (Lausanne), 2021, 8:788663 Int J Pharm, 2019, 570:118661
S3868	Harmine	Harmine (Telepathine), a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds, is a highly cell-permeant and competitive inhibitor of ATP binding to the kinase pocket of DYRK1A, with about 60-fold higher IC50 value for DYRK2. Harmine also inhibits monoamine oxidases (MAOs), PPARγ and cdc-like kinases (CLKs). Harmine inhibits 5-HT2A serotonin receptor with Ki of 397 nM.	J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493 Cell Death Dis, 2019, 10(12):899
S4708	Palmitoylethanolamide	Palmitoylethanolamide (PEA, Palmidrol, N-palmitoylethanolamine) is an endogenous fatty acid amide and selectively activates PPAR-α in vitro with an EC50 value of 3.1±0.4 μM.	Nat Commun, 2024, 15(1):8221 Neurosci Insights, 2020, 15:2633105520975412 J Steroid Biochem Mol Biol, 2019, 10.1016/j.jsbmb.2018.07.005
S2665	Ciprofibrate	Ciprofibrate (Win-35833) is a peroxisome proliferator-activated receptor agonist.	Respir Physiol Neurobiol, 2020, 271:103290
S1849	Daidzein	Daidzein is a natural isoflavone phytoestrogen found in Leguminosae, used as a component of foods and dietary supplements. Daidzein is a soy isoflavone, which acts as a PPAR activator.	Ecotoxicol Environ Saf, 2024, 275:116262 J Mol Neurosci, 2018, 64(2):211-223
S4207	Clofibric Acid	Clofibric acid(Chlorofibrinic acid) is a PPARα agonist and hypolipidemic agent.	Lab Invest, 2023, 103(1):100004
S8770	Lanifibranor (IVA-337)	Lanifibranor (IVA-337) is a moderately potent and well balanced pan PPAR agonist with EC50 values of 1537 nM, 866 nM and 206 nM for hPPARα, hPPARδ and hPPARγ, respectively.	Brain Res Bull, 2021, 177:22-30
S0531	DG172 dihydrochloride	DG-172 dihydrochloride is a novel PPARβ/δ-selective antagonist with the IC50 of 27 nM.	Cell Signal, 2022, 93:110304
S6906	Capric acid	Capric acid (DA, Decanoic acid, Decylic acid), a component of medium-chain triclycerides occurring naturally in coconut oil and palm kernel oil, contributes to seizure control through direct AMPA receptor inhibition. Capric acid is also a modulating ligand for PPARs. Due to its specific melting range the product may be solid, liquid, a solidified melt or a supercooled melt.	Pharmaceuticals (Basel), 2023, 16(5)692
S3786	Glabridin	Glabridin (Q-100692, KB-289522, LS-176045), one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory.	Life Sci, 2021, S0024-3205(20)31752-5
S3875	Alpinetin	Alpinetin, a composition of Alpinia katsumadai Hayata, has been reported to have a number of biological properties, such as antibacterial, antitumor and other important therapeutic activities. Alpinetin is a flavonoid isolated from Alpinia katsumadai Hayata, activates activates PPAR-γ, with potent anti-inflammatory activity.	Nutrients, 2021, 13(10)3382
S3720	Elafibranor	Elafibranor (GFT505) is an agonist of the peroxisome proliferator-activated receptor-α(PPAR-alpha) and peroxisome proliferator-activated receptor-δ(PPAR-δ). It improves insulin sensitivity, glucose homeostasis, and lipid metabolism and reduces inflammation.	JHEP Rep, 2023, 5(10):100845 JHEP Rep, 2023, 5(10):100845
S7867	Oleuropein	Oleuropein is an antioxidant polyphenol isolated from olive leaf. Oleuropein exerts antioxidant, anti-inflammatory and anti-atherogenic effects and suppresses the adipocyte differentiation in vitro. Oleuropein inhibits PPARγ activity. Oleuropein exerts anti-adipogenic effect through direct inhibition of PPARγ transcriptional activity. Oleuropein also inhibits aromatase. Oleuropein induces apoptosis. Phase 2.	Front Endocrinol (Lausanne), 2024, 15:1354435 J Med Virol, 2019, 91(8):1440-1447
S9177	Gypenoside XLIX	Gypenoside XLIX, a naturally occurring gynosaponin, is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator.	Chin Med, 2024, 19(1):70 Am J Transl Res, 2023, 15(2):834-846
S1473^New	GW501516	GW501516 is a potent and highly selective PPARβ/δ agonist, with EC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ. Phase 4.
S1729	Gemfibrozil	Gemfibrozil (CI-719) is an activator of peroxisome proliferator-activated receptor-alpha (PPARα), used for the treatment of hypercholesterolemia and hypertriglyceridemia.	J Immunother Cancer, 2024, 12(11)e009805
S9199	Pseudoginsenoside F11	Pseudoginsenoside F11, a natural product found in American ginseng but not in Asian ginseng, is a novel partial PPARγ agonist.
S3290	Procyanidin B2 (PCB2)	Procyanidin B2 (PCB2), a natural flavonoid found in commonly consumed foods, possess anti-inflammatory, anti-oxidant and anti-cancer activities. Procyanidin B2 activates PPARγ to induce M2 polarization in mouse macrophages. Procyanidin B2 significantly suppresses the activation of NLRP3 inflammasome in the lung tissue induced by paraquat in the rat model.	BMC Cardiovasc Disord, 2024, 24(1):231 Front Pharmacol, 2021, 12:639651
E0473	CUDA	CUDA is a potent inhibitor of soluble epoxide hydrolase (sEH), with IC50s of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively, also selectively increases peroxisome proliferator-activated receptor (PPAR) alpha activity.
S5121	Phytol	Phytol (Trans-Phytol), a diterpene alcohol from chlorophyll widely used as a food additive and in medicinal fields, shows antinociceptive and antioxidant activities as well as anti-inflammatory and antiallergic effects. It is a specific activator of PPARα.
S0773	Mifobate	Mifobate (SR-202), a potent and specific PPARγ antagonist, selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM).
E2876	pemafibrate	Pemafibrate(K-877) is a selective agonist of peroxisome proliferator-activated receptor (PPAR) α with an IC50 of 10 µM.
E3521	Auricledleaf Swallowwort Root Extract	Auricledleaf Swallowwort Root Extract is obtained from Cynanchum otophyllum Schneid., which may be mediated by activation of PPARα and TFEB, and the subsequent autophagy-lysosomal pathway enhancement, thus attenuate Alzheimer’s disease pathology and improve cognitive function in 3XTg mice.
S8046	GW7647	GW7647 is a potent PPARα agonist, with EC50s of 6 nM, 1.1 μM, and 6.2 μM for human PPARα, PPARγ and PPARδ, respectively.
S6635^New	Seladelpar	Seladelpar(MBX-8025) is a potent and selective agonist of peroxisome proliferator–activated receptor-delta (PPAR-δ) with EC50 of 2 nM for human PPAR-δ. MBX-8025 enhances insulin sensitivity, counters dyslipidemia, and reduces hepatic storage of lipotoxic lipids, thereby ameliorating NASH pathology in obese diabetic mice.
S5824	Cinnamyl alcohol	Cinnamyl alcohol is a naturally occurring compound that is found within cinnamon. Cinnamyl alcohol can be significantly attenuated the enhanced expression of obesity-related proteins PPARγ in MDI medium-cultivated 3T3-L1 cells.
S5113	Propyl gallate	Propyl gallate (Gallic acid propyl esterZ, n-Propyl gallate) is an antioxidant used in foods especially animal fats and vegetable oils, also in a wide variety of cosmetics and beauty care products.
S3878	Bavachinin	Bavachinin (7-O-Methylbavachin) is a novel natural pan-PPAR agonist from the fruit of the traditional Chinese glucose-lowering herb malaytea scurfpea. It shows stronger activities with PPAR-γ than with PPAR-α and PPAR-β/δ (EC50 = 0.74 μmol/l, 4.00 μmol/l and 8.07 μmol/l in 293T cells, respectively).
S0170	BMS-687453	BMS-687453 (compound 2) is a potent and selective agonist of PPARα with EC50 of 10 nM and IC50 of 260 nM for human PPARα.
S5812	Choline Fenofibrate	Choline fenofibrate(ABT-335) is a newly developed choline salt of fenofibric acid, a synthetic phenoxy-isobutyric acid derivate with antihyperlipidemic activity that acts as an PPARα agonist.
S9674	Saroglitazar	Saroglitazar (Lipaglyn, ZYH1) is an agonist of peroxisome proliferator-activated receptor (PPAR) with EC50 of 0.65 pM and 3 nM for hPPARα and hPPARγ in HepG2 cells, respectively.
E1699^New	SR10221	SR10221 is a inverse-agonist of PPARγ with IC50 of 1.6 nM in RT112/84 FABP4-NLucP reporter assay. It exhibits an antiproliferative activity in vitro.
S9129	20(S)-Ginsenoside Rh1	20(S)-Ginsenoside Rh1 (Prosapogenin A2, Sanchinoside B2, Sanchinoside Rh1) is one of major bioactive compounds extracted from red ginseng, which has been increasingly used for enhancing cognition and physical health worldwide. It exhibits potent characteristics of anti-inflammatory, antioxidant, immunomodulatory effects, and positive effects on the nervous system. Ginsenoside Rh1 inhibits the expression of PPAR-γ, TNF-α, IL-6, and IL-1β.
S9480	Raspberry Ketone	Raspberry ketone (p-Hydroxybenzyl acetone, Frambinone, Oxyphenylon, Rheosmin, Rasketone) is a natural phenolic compound that is the primary aroma compound of red raspberries. Raspberry ketone shows cardioprotective action against isoproterenol-induced myocardial infarction in rats, and the effects may be due to its PPAR-α agonistic activity.
S5851	4'-Methoxychalcone	4'-Methoxychalcone, found in citrus, is chalcone derivative that has shown diverse pharmacological properties, including anti-tumor and anti-inflammatory activities. 4'-Methoxychalcone significantly enhanced adipocyte differentiation, in part, by its potent effects on PPARγ activation and by its reverse effect on TNF-α.
E1775^New	2,4-Thiazolidinedione	2,4-Thiazolidinedione (Thiazolidinedione), an insulin sensitizer, is a specific agonist of peroxisome proliferator-activated receptor (PPAR)γ. Thiazolidinedione treatment corrects impaired muscle insulin action in vivo.
E1831^New	FX-909	FX-909 is an orally available inverse agonist and inhibitor of the transcription factor (TF) peroxisome proliferator activated receptor gamma (PPARG, PPARγ) ), which exhibits anti-tumor activity in vivo.
S2871	T0070907	T0070907 is a potent inhibitor of PPARγ (peroxisome proliferator activator receptor γ ) that induces G2/M arrest and enhances the effect of radiation in human cervical cancer cells through mitotic catastrophe. It also acts as an antagonist of PPARγ that suppresses breast cancer cell proliferation and motility via both PPARgamma-dependent and -independent mechanisms.	Immunity, 2024, 57(10):2344-2361.e7 Nat Commun, 2024, 15(1):1429 Bone Res, 2024, 12(1):15
S7484	FH535	FH535 is a Wnt/β-catenin signaling inhibitor and also a dual PPARγ and PPARδ antagonist.	Int J Biol Sci, 2024, 20(6):2323-2338 Gastroenterology, 2023, S0016-5085(23)00114-2 Gastroenterology, 2023, 164(6):990-1005
S2798	GW6471	GW 6471 is a potent antagonist of PPARα with IC50 of 0.24 μM.	Nat Commun, 2024, 15(1):7611 Cancer Lett, 2024, 587:216724 JCI Insight, 2024, 9(6)e171961
S7767	AZ6102	AZ6102 is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows IC50 of 5 nM for Wnt pathway inhibition in DLD-1 cells.	Nat Commun, 2022, 13(1):2070 Sci Adv, 2022, 8(19):eabh2332 Haematologica, 2021, 10.3324/haematol.2020.267096
S4527	Fenofibric acid	Fenofibric acid (NSC 281318, Trilipix, FNF acid) is a fibrate that acts as a lipid-lowering agent, decreasing low-density lipoprotein cholesterol and triglycerides.	J Immunother Cancer, 2024, 12(11)e009805 Front Med (Lausanne), 2021, 8:788663 Int J Pharm, 2019, 570:118661
S7867	Oleuropein	Oleuropein is an antioxidant polyphenol isolated from olive leaf. Oleuropein exerts antioxidant, anti-inflammatory and anti-atherogenic effects and suppresses the adipocyte differentiation in vitro. Oleuropein inhibits PPARγ activity. Oleuropein exerts anti-adipogenic effect through direct inhibition of PPARγ transcriptional activity. Oleuropein also inhibits aromatase. Oleuropein induces apoptosis. Phase 2.	Front Endocrinol (Lausanne), 2024, 15:1354435 J Med Virol, 2019, 91(8):1440-1447
S5824	Cinnamyl alcohol	Cinnamyl alcohol is a naturally occurring compound that is found within cinnamon. Cinnamyl alcohol can be significantly attenuated the enhanced expression of obesity-related proteins PPARγ in MDI medium-cultivated 3T3-L1 cells.
S5113	Propyl gallate	Propyl gallate (Gallic acid propyl esterZ, n-Propyl gallate) is an antioxidant used in foods especially animal fats and vegetable oils, also in a wide variety of cosmetics and beauty care products.
S9129	20(S)-Ginsenoside Rh1	20(S)-Ginsenoside Rh1 (Prosapogenin A2, Sanchinoside B2, Sanchinoside Rh1) is one of major bioactive compounds extracted from red ginseng, which has been increasingly used for enhancing cognition and physical health worldwide. It exhibits potent characteristics of anti-inflammatory, antioxidant, immunomodulatory effects, and positive effects on the nervous system. Ginsenoside Rh1 inhibits the expression of PPAR-γ, TNF-α, IL-6, and IL-1β.
S8029	WY-14643 (Pirinixic Acid)	WY-14643 (Pirinixic Acid, NSC 310038) is a potent and selective PPARα activator with an EC50 of 1.5 μM.	Front Pharmacol, 2024, 15:1366479 Front Pharmacol, 2024, 15:1366479 Cell Mol Gastroenterol Hepatol, 2022, 14(6):1311-1331
S9189	Oroxin A	Oroxin A (Baicalein 7-O-glucoside), an active component isolated from the herb Oroxylum indicum (L.) Kurz, activates PPARγ and inhibits α-glucosidase, exerting antioxidant activity.	Front Pharmacol, 2022, 13:894899 An Acad Bras Cienc, 2022, 94(suppl 4):e20211400
S9723	CDDO-Im (RTA-403)	CDDO-Im (RTA-403) is an activator of nuclear factor erythroid 2–related factor 2 (Nrf2) and peroxisome proliferator-activated receptor (PPAR). CDDO-Im binds to PPARα and PPARγ with Ki of 232 nM and 344 nM, respectively. CDDO-Im inhibits inflammatory response and tumor growth in vivo.	Ecotoxicol Environ Saf, 2022, 241:113754 Int J Mol Sci, 2022, 23(19)11715
S4708	Palmitoylethanolamide	Palmitoylethanolamide (PEA, Palmidrol, N-palmitoylethanolamine) is an endogenous fatty acid amide and selectively activates PPAR-α in vitro with an EC50 value of 3.1±0.4 μM.	Nat Commun, 2024, 15(1):8221 Neurosci Insights, 2020, 15:2633105520975412 J Steroid Biochem Mol Biol, 2019, 10.1016/j.jsbmb.2018.07.005
S1849	Daidzein	Daidzein is a natural isoflavone phytoestrogen found in Leguminosae, used as a component of foods and dietary supplements. Daidzein is a soy isoflavone, which acts as a PPAR activator.	Ecotoxicol Environ Saf, 2024, 275:116262 J Mol Neurosci, 2018, 64(2):211-223
S3875	Alpinetin	Alpinetin, a composition of Alpinia katsumadai Hayata, has been reported to have a number of biological properties, such as antibacterial, antitumor and other important therapeutic activities. Alpinetin is a flavonoid isolated from Alpinia katsumadai Hayata, activates activates PPAR-γ, with potent anti-inflammatory activity.	Nutrients, 2021, 13(10)3382
S9177	Gypenoside XLIX	Gypenoside XLIX, a naturally occurring gynosaponin, is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator.	Chin Med, 2024, 19(1):70 Am J Transl Res, 2023, 15(2):834-846
S1729	Gemfibrozil	Gemfibrozil (CI-719) is an activator of peroxisome proliferator-activated receptor-alpha (PPARα), used for the treatment of hypercholesterolemia and hypertriglyceridemia.	J Immunother Cancer, 2024, 12(11)e009805
S3290	Procyanidin B2 (PCB2)	Procyanidin B2 (PCB2), a natural flavonoid found in commonly consumed foods, possess anti-inflammatory, anti-oxidant and anti-cancer activities. Procyanidin B2 activates PPARγ to induce M2 polarization in mouse macrophages. Procyanidin B2 significantly suppresses the activation of NLRP3 inflammasome in the lung tissue induced by paraquat in the rat model.	BMC Cardiovasc Disord, 2024, 24(1):231 Front Pharmacol, 2021, 12:639651
E0473	CUDA	CUDA is a potent inhibitor of soluble epoxide hydrolase (sEH), with IC50s of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively, also selectively increases peroxisome proliferator-activated receptor (PPAR) alpha activity.
S5121	Phytol	Phytol (Trans-Phytol), a diterpene alcohol from chlorophyll widely used as a food additive and in medicinal fields, shows antinociceptive and antioxidant activities as well as anti-inflammatory and antiallergic effects. It is a specific activator of PPARα.
E3521	Auricledleaf Swallowwort Root Extract	Auricledleaf Swallowwort Root Extract is obtained from Cynanchum otophyllum Schneid., which may be mediated by activation of PPARα and TFEB, and the subsequent autophagy-lysosomal pathway enhancement, thus attenuate Alzheimer’s disease pathology and improve cognitive function in 3XTg mice.
S5851	4'-Methoxychalcone	4'-Methoxychalcone, found in citrus, is chalcone derivative that has shown diverse pharmacological properties, including anti-tumor and anti-inflammatory activities. 4'-Methoxychalcone significantly enhanced adipocyte differentiation, in part, by its potent effects on PPARγ activation and by its reverse effect on TNF-α.
S2915	GW9662	GW9662 is a selective PPAR antagonist for PPARγ with IC50 of 3.3 nM in a cell-free assay, with at least 10- to 600-fold functional selectivity in cells with PPARγ versus PPARα and PPARδ.	J Hematol Oncol, 2024, 17(1):9 Research (Wash D C), 2024, 7:0400 Int J Biol Sci, 2024, 20(6):2323-2338
S8025	GSK3787	GSK3787 is a selective and irreversible antagonist of PPARδ with pIC50 of 6.6, with no measurable affinity for hPPARα or hPPARγ.	Drug Des Devel Ther, 2024, 18:4799-4824 Cell Discov, 2023, 9(1):54 Cell Discov, 2023, 9(1):54
S5817	GSK0660	GSK0660 is a potent PPARβ/δ antagonist with a pIC50 of 6.8 (binding assay IC50 = 155 nM; antagonist assay IC50 = 300 nM) and is nearly inactive on PPARα and PPARγ with IC50s above approximately 10 μM.	Cells, 2024, 13(3):206. Cells, 2024, 13(3)206 Elife, 2023, 12e82970
S0531	DG172 dihydrochloride	DG-172 dihydrochloride is a novel PPARβ/δ-selective antagonist with the IC50 of 27 nM.	Cell Signal, 2022, 93:110304
S0773	Mifobate	Mifobate (SR-202), a potent and specific PPARγ antagonist, selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM).
S2556	Rosiglitazone	Rosiglitazone is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action. Rosiglitazone modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.	Nat Commun, 2024, 15(1):1429 Nat Commun, 2024, 15(1):7991 Research (Wash D C), 2024, 7:0400
S2590	Pioglitazone	Pioglitazone is a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist, used to treat diabetes; A weak activator for full-length hPPARα, but not full-length hPPARδ.	Signal Transduct Target Ther, 2024, 9(1):257 Cell Commun Signal, 2024, 22(1):266 Braz J Med Biol Res, 2024, 57:e13235
S2505	Rosiglitazone maleate	Rosiglitazone maleate, a member of the thiazolidinedione class of antihyperglycaemic agents, is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ (PPAR-γ) with IC50 of 42 nM. Rosiglitazone maleate also modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.	Stem Cell Reports, 2022, 17(11):2531-2547 Cell Death Dis, 2021, 12(11):972 Antioxidants (Basel), 2021, 10(2)155
S2075	Rosiglitazone HCl	Rosiglitazone HCl is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.	J Immunother Cancer, 2024, 12(11)e009805 Stem Cell Reports, 2022, 17(11):2531-2547 Cell Death Dis, 2021, 12(11):972
S1794	Fenofibrate	Fenofibrate is a compound of the fibrate class and fibric acid derivative. Fenofibrate is a selective agonist of PPARα with EC50 of 30 μM. Fenofibrate binds to and inhibits cytochrome P450 epoxygenase (CYP)2C with IC50 of 0.2 μM, 0.7 μM and 9.7 μM for CYP2C19, CYP2B6 and CYP2C9, respectively. Fenofibrate induces autophagy.	J Immunother Cancer, 2024, 12(11)e009805 Heliyon, 2024, 10(11):e31861 Cancer Lett, 2023, 10.1016/j.canlet.2023.216427
S2046	Pioglitazone HCl	Pioglitazone HCl (AD-4833, U-72107E) is an inhibitor of cytochrome P450 (CYP)2C8 and CYP3A4 enzymes. Pioglitazone HCl inhibits CYP2C8, CYP3A4 and CYP2C9 with Ki of 1.7 μM, 11.8 μM and 32.1 μM, respectively. Pioglitazone HCl is also a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist with EC50 of 0.93 μM and 0.99 μM for human PPARγ and mouse PPARγ, respectively. Pioglitazone HCl inhibits mitochondrial iron uptake, lipid peroxidation, and subsequent ferroptosis.	J Transl Med, 2024, 22(1):593 Commun Biol, 2022, 5(1):231 J Genet Genomics, 2022, S1673-8527(22)00133-3
S8020	GW0742	GW0742 is a potent and highly selective PPARβ/δ agonist, with IC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ.	Cell Commun Signal, 2024, 22(1):266 Med Oncol, 2024, 41(8):188 Life Sci, 2021, 279:119696
S3846	Eupatilin	Eupatilin (NSC 122413), a major flavonoid from Artemisia plants, possesses various beneficial biological effects including anti-inflammation, anti-tumor, anti-cancer, anti-allergy, and anti-oxidation activity. Eupatilin, a lipophilic flavonoid isolated from Artemisia species, is a PPARα agonist, and possesses anti-apoptotic, anti-oxidative and anti-inflammatory activities.	Int J Mol Sci, 2023, 24(6)5933 Front Pharmacol, 2022, 13:940475 Int J Mol Sci, 2022, 23(24)16055
S8432	Troglitazone	Troglitazone is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR) that is a ligand activated transcription factor regulating cell differentiation and growth. Troglitazone induces autophagy, apoptosis and necroptosis in bladder cancer cells. Troglitazone prevents RSL3-induced ferroptosis and lipid peroxidation in Pfa1 cells.	CNS Neurosci Ther, 2024, 30(8):e14911 Int J Mol Med, 2024, 53(4)37 Free Radic Biol Med, 2021, 163:234-242
S4159	Bezafibrate	Bezafibrate (BM 15075) is the first clinically tested dual and pan-PPAR co-agonism.	Nat Commun, 2021, 12(1):1929 PPAR Res, 2021, 2021:5589342
S2665	Ciprofibrate	Ciprofibrate (Win-35833) is a peroxisome proliferator-activated receptor agonist.	Respir Physiol Neurobiol, 2020, 271:103290
S4207	Clofibric Acid	Clofibric acid(Chlorofibrinic acid) is a PPARα agonist and hypolipidemic agent.	Lab Invest, 2023, 103(1):100004
S8770	Lanifibranor (IVA-337)	Lanifibranor (IVA-337) is a moderately potent and well balanced pan PPAR agonist with EC50 values of 1537 nM, 866 nM and 206 nM for hPPARα, hPPARδ and hPPARγ, respectively.	Brain Res Bull, 2021, 177:22-30
S3786	Glabridin	Glabridin (Q-100692, KB-289522, LS-176045), one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory.	Life Sci, 2021, S0024-3205(20)31752-5
S3720	Elafibranor	Elafibranor (GFT505) is an agonist of the peroxisome proliferator-activated receptor-α(PPAR-alpha) and peroxisome proliferator-activated receptor-δ(PPAR-δ). It improves insulin sensitivity, glucose homeostasis, and lipid metabolism and reduces inflammation.	JHEP Rep, 2023, 5(10):100845 JHEP Rep, 2023, 5(10):100845
S1473^New	GW501516	GW501516 is a potent and highly selective PPARβ/δ agonist, with EC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ. Phase 4.
S9199	Pseudoginsenoside F11	Pseudoginsenoside F11, a natural product found in American ginseng but not in Asian ginseng, is a novel partial PPARγ agonist.
E2876	pemafibrate	Pemafibrate(K-877) is a selective agonist of peroxisome proliferator-activated receptor (PPAR) α with an IC50 of 10 µM.
S8046	GW7647	GW7647 is a potent PPARα agonist, with EC50s of 6 nM, 1.1 μM, and 6.2 μM for human PPARα, PPARγ and PPARδ, respectively.
S6635^New	Seladelpar	Seladelpar(MBX-8025) is a potent and selective agonist of peroxisome proliferator–activated receptor-delta (PPAR-δ) with EC50 of 2 nM for human PPAR-δ. MBX-8025 enhances insulin sensitivity, counters dyslipidemia, and reduces hepatic storage of lipotoxic lipids, thereby ameliorating NASH pathology in obese diabetic mice.
S3878	Bavachinin	Bavachinin (7-O-Methylbavachin) is a novel natural pan-PPAR agonist from the fruit of the traditional Chinese glucose-lowering herb malaytea scurfpea. It shows stronger activities with PPAR-γ than with PPAR-α and PPAR-β/δ (EC50 = 0.74 μmol/l, 4.00 μmol/l and 8.07 μmol/l in 293T cells, respectively).
S0170	BMS-687453	BMS-687453 (compound 2) is a potent and selective agonist of PPARα with EC50 of 10 nM and IC50 of 260 nM for human PPARα.
S5812	Choline Fenofibrate	Choline fenofibrate(ABT-335) is a newly developed choline salt of fenofibric acid, a synthetic phenoxy-isobutyric acid derivate with antihyperlipidemic activity that acts as an PPARα agonist.
S9674	Saroglitazar	Saroglitazar (Lipaglyn, ZYH1) is an agonist of peroxisome proliferator-activated receptor (PPAR) with EC50 of 0.65 pM and 3 nM for hPPARα and hPPARγ in HepG2 cells, respectively.
E1699^New	SR10221	SR10221 is a inverse-agonist of PPARγ with IC50 of 1.6 nM in RT112/84 FABP4-NLucP reporter assay. It exhibits an antiproliferative activity in vitro.
S9480	Raspberry Ketone	Raspberry ketone (p-Hydroxybenzyl acetone, Frambinone, Oxyphenylon, Rheosmin, Rasketone) is a natural phenolic compound that is the primary aroma compound of red raspberries. Raspberry ketone shows cardioprotective action against isoproterenol-induced myocardial infarction in rats, and the effects may be due to its PPAR-α agonistic activity.
E1775^New	2,4-Thiazolidinedione	2,4-Thiazolidinedione (Thiazolidinedione), an insulin sensitizer, is a specific agonist of peroxisome proliferator-activated receptor (PPAR)γ. Thiazolidinedione treatment corrects impaired muscle insulin action in vivo.
E1831^New	FX-909	FX-909 is an orally available inverse agonist and inhibitor of the transcription factor (TF) peroxisome proliferator activated receptor gamma (PPARG, PPARγ) ), which exhibits anti-tumor activity in vivo.
S7955	EPI-001	EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.	Int J Biol Macromol, 2024, 278(Pt 3):134844 Nat Struct Mol Biol, 2023, 30(12):1958-1969 Int J Mol Sci, 2023, 24(4)3823
S3834	Astaxanthin	Astaxanthin (β-Carotene-4,4'-dione, Trans-Astaxanthin), a xanthophyll carotenoid, is a nutrient with unique cell membrane actions and diverse clinical benefits with excellent safety and tolerability. Astaxanthin, a red dietary carotenoid isolated from Haematococcus pluvialis, is a modulator of PPARγ and a potent antioxidant with antiproliferative, neuroprotective and anti-inflammatory activity.	Int Immunopharmacol, 2023, 119:110159 J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493 Aging (Albany NY), 2019, 11(22):10513-10531
S3868	Harmine	Harmine (Telepathine), a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds, is a highly cell-permeant and competitive inhibitor of ATP binding to the kinase pocket of DYRK1A, with about 60-fold higher IC50 value for DYRK2. Harmine also inhibits monoamine oxidases (MAOs), PPARγ and cdc-like kinases (CLKs). Harmine inhibits 5-HT2A serotonin receptor with Ki of 397 nM.	J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493 Cell Death Dis, 2019, 10(12):899
S6906	Capric acid	Capric acid (DA, Decanoic acid, Decylic acid), a component of medium-chain triclycerides occurring naturally in coconut oil and palm kernel oil, contributes to seizure control through direct AMPA receptor inhibition. Capric acid is also a modulating ligand for PPARs. Due to its specific melting range the product may be solid, liquid, a solidified melt or a supercooled melt.	Pharmaceuticals (Basel), 2023, 16(5)692
S1473^New	GW501516	GW501516 is a potent and highly selective PPARβ/δ agonist, with EC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ. Phase 4.
S6635^New	Seladelpar	Seladelpar(MBX-8025) is a potent and selective agonist of peroxisome proliferator–activated receptor-delta (PPAR-δ) with EC50 of 2 nM for human PPAR-δ. MBX-8025 enhances insulin sensitivity, counters dyslipidemia, and reduces hepatic storage of lipotoxic lipids, thereby ameliorating NASH pathology in obese diabetic mice.
E1699^New	SR10221	SR10221 is a inverse-agonist of PPARγ with IC50 of 1.6 nM in RT112/84 FABP4-NLucP reporter assay. It exhibits an antiproliferative activity in vitro.
E1775^New	2,4-Thiazolidinedione	2,4-Thiazolidinedione (Thiazolidinedione), an insulin sensitizer, is a specific agonist of peroxisome proliferator-activated receptor (PPAR)γ. Thiazolidinedione treatment corrects impaired muscle insulin action in vivo.
E1831^New	FX-909	FX-909 is an orally available inverse agonist and inhibitor of the transcription factor (TF) peroxisome proliferator activated receptor gamma (PPARG, PPARγ) ), which exhibits anti-tumor activity in vivo.

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