S3003 |
Prostaglandin E2 (PGE2)
|
Prostaglandin E2 (PGE2, Dinoprostone) plays important effects in labour (softens cervix and causes uterine contraction) and also stimulates osteoblasts to release factors that stimulate bone resorption by osteoclasts.
|
-
J Exp Clin Cancer Res, 2024, 43(1):277
-
Front Pharmacol, 2024, 15:1372109
-
bioRxiv, 2024, 2024.07.12.603155
|
|
S7211 |
PF-04418948
|
PF-04418948 is a potent and selective prostaglandin EP₂ receptor antagonist with IC50 of 16 nM. Phase 1.
|
-
Int J Mol Sci, 2023, 24(13)10881
-
Cancer Res Commun, 2023, 3(8):1486-1500
-
Cancer Res Commun, 2023, 3(8):1486-1500
|
|
S6793 |
TG4-155
|
TG4-155 is a potent and selective Prostaglandin Receptor EP2(PTGER2) antagonist with Ki value of 9.9 nM. |
-
Elife, 2023, 12e81438
-
Elife, 2023, 12e81438
-
bioRxiv, 2021, 10.1101/2021.08.27.457936
|
|
S1407 |
Bimatoprost
|
Bimatoprost(AGN 192024) is a prostaglandin analog used topically (as eye drops) to control the progression of glaucoma and in the management of ocular hypertension. |
-
PLoS Pathog, 2020, 16;16(3):e1008341
-
Invest Ophthalmol Vis Sci, 2018, 59(15):5912-5923
|
|
S3726 |
Selexipag
|
Selexipag (NS-304, ACT-293987) is an orally active, first-in-class, selective prostacyclin IP receptor agonist with Ki value of 260 nM for human IP, whereas Ki values > 10,000 nM are measured at the other human G-protein-coupled prostanoid receptors (EP1-4, DP, FP and TP). |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Biol Pharm Bull, 2022, 10.1248/bpb.b21-01057
-
Front Med (Lausanne), 2021, 8:742436
|
|
S6649 |
E7046 (ER-886406)
|
E7046 (ER-886406, Palupiprant, AN0025) is a selective inhibitor of the prostaglandin E2 (PGE2) receptor EP4 with IC50 of 13.5 nM and Ki of 23.14 nM. |
-
Cell Mol Life Sci, 2022, 79(6):303
|
|
S6694 |
Grapiprant (CJ-023,423)
|
Grapiprant (CJ-023,423, AT-001, AAT-007, RQ-00000007, CJ-23423) is a novel selective EP4 Prostaglandin Receptor inhibitor with Ki of 20 nM and 13 nM for rat EP4 receptor and human EP4 receptor, respectively. |
-
Bone Res, 2022, 10(1):27
|
|
S3346 |
1-Methylnicotinamide chloride
|
1-Methylnicotinamide (1-MNA, 3-Carbamoyl-1-methylpyridin-1-ium, Trigonellamide) chloride is an active endogenous metabolite of nicotinamide that exhibits anti-inflammatory and anti-thrombotic activities. 1-Methylnicotinamide enhances tumor vasculature formation and markedly increases prostacyclin (PGI2) generation. |
-
Oncol Rep, 2021, 45(6)110
|
|
S0141 |
NQ301
|
NQ301 (Compound 211), an antiplatelet and antithrombotic agent, is a selective CD45 inhibitor with IC50 of 200 nM. NQ301 inhibits thromboxane A2 receptor (TXA2) and synthase activity in rabbit platelets. |
-
J Extracell Vesicles, 2021, 10(5):e12078
|
|
S2496 |
Ozagrel
|
Ozagrel (OKY-046) is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia. |
|
|
S2067 |
Ozagrel HCl
|
Ozagrel HCl (OKY-046) is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia. |
|
|
S0495 |
BI-671800
|
BI-671800 (AP-761, Cmpd A) is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2) with IC50 of 4.5 nM and 3.7 nM for PGD2 binding to human CRTH2 and murine CRTH2, respectively. BI-671800 is associated with a small improvement in FEV1 in symptomatic controller-naïve asthma patients, and in patients on ICS. |
|
|
S5753 |
Setipiprant (ACT-129968)
|
Setipiprant (ACT-129968, KYTH-105) is a selective, orally available antagonist of the prostaglandin D2 receptor 2 (DP2) that that has been shown to have greater specificity for DP2 (CRTH2) than for DP1. |
|
|
S4851 |
Tafluprost
|
Tafluprost (AFP-168,MK2452) is a novel prostaglandin analog with a high affinity for the fluoroprostaglandin (FP) receptor PGF2α. A prostanoid selective FP receptor agonist. |
|
|
S6496 |
Genz-123346 free base
|
Genz-123346 is an inhibitor of GL1 synthase that blocks the conversion of ceramide to GL1, the first step in the biosynthesis of gangliosides and other glycosphingolipids. |
|
|
E1477 |
EP4-IN-1
|
EP4-IN-1 is a potent prostanoid EP4 receptor inhibitor. It exhibits prospects in tumor immunity and anti-inflammatory analgesia research. |
|
|
S5252 |
Ozagrel sodium
|
Ozagrel sodium (KCT-0809, Cataclot, Xanbo) is a thromboxane A2 synthase (CYP5) inhibitor with neuroprotective properties. |
|
|
S0541 |
Dazoxiben hydrochloride
|
Dazoxiben hydrochloride (HCl) is a potent, selevtive and orally active inhibitor of thromboxane (TX) synthase. Dazoxiben inhibits TXB2 production in clotting human whole blood with IC50 of 0.3 μM and causes parallel enhancement of PGE2 production. |
|
|
S5594 |
α-Terpineol
|
α-Terpineol, a natural monoterpene, is the major component of essential oils of several species of aromatic plants such as Origanium vulgare L. and Ocimum canum Sims which are widely used for medicinal purposes. It is widely used in the manufacturing of cosmetics, soaps, perfumes, antiseptic agents and is considered one of the most frequently used fragrance compounds. α-TPN has anticholinergic action and can block the interaction between PGE2 and GM1 receptors and cholera toxin. |
|
|
S0305 |
RO1138452
|
RO1138452 (CAY10441) is a potent and selective antagonist of IP (prostacyclin, PGI2) receptor with pKi of 9.3 and 8.7 in human platelets and a recombinant IP receptor system, respectively. |
|
|
S5286 |
Ramatroban
|
Ramatroban (BAY u 3405) is a thromboxane A2(TxA2) receptor antagonist with Ki value of 10 to 13 nM. It also antagonizes a newly identified PGD2 receptor, CRTh2 expressed on the inflammatory cells. |
|
|
E2873 |
Laropiprant
|
Laropiprant is a potent and selective prostaglandin D2 (DP) receptor antagonist with a Ki value of 0.57 nM.
|
|
|
S4152 |
Ethamsylate
|
Ethamsylate (Etamsylate) is a haemostatic drug, which inhibits biosynthesis and action of prostaglandins, and increases capillary endothelial resistance as and platelet adhesion. |
-
J Immunother Cancer, 2024, 12(11)e009805
|
|
S9327 |
Carboprost
|
Carboprost is a synthetic prostaglandin analogue of PGF2α with oxytocic properties. |
|
|
S0325 |
Treprostinil sodium
|
Treprostinil sodium is a potent agonist of DP1, EP2 and IP receptors with Ki 4.4 nM, 3.6 nM and 32 nM, respectively. |
|
|
S0099 |
Asapiprant
|
Asapiprant(S-555739) is a potent and selective DP1 receptor antagonist with a Ki of 0.44 nM, which has potential as a novel therapy for allergic airway diseases. |
|
|
E4846New |
Treprostinil
|
Treprostinil is a potent agonist of DP1 and EP2 with EC50 of 0.6 nM and 6.2 nM for DP1 and EP2 receptors, respectively. It is a vasodilator used to treat pulmonary arterial hypertension and improves mitochondrial impairment in vitro. |
|
|
E0612 |
MF-766
|
MF-766 is a highly potent, selective and orally active EP4 antagonist with a Ki of 0.23 nM. |
|
|
S0111 |
Taprenepag
|
Taprenepag(CP-544326) is a potent and selective prostaglandin EP2 agonist with IC50s of 10 and 15 nM for human and rat EP2, respectively. |
|
|
E0053 |
Evatanepag
|
Evatanepag (CP-533536 free acid) is a potent and selective EP2 receptor agonist with an IC50 of 50 nM for rEP2.
|
|
|
S5819 |
MRE-269 (ACT-333679)
|
MRE-269 (ACT-333679) is a prostaglandin I2 (IP) receptor agonist with a binding affinity for the human IP receptor that is 130-fold greater than that for other human prostanoid receptor. |
|
|
E0809 |
Timapiprant Sodium
|
Timapiprant sodium (OC000459 sodium), a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist, potently displaces [3H]PGD2 from human recombinant DP2, rat recombinant DP2, and human native DP2 with Ki values of 13, 3 and 4 nM, respectively. |
|
|
E2986 |
ONO-AE3-208
|
ONO-AE3-208(AE 3-208) is a selective and orally active EP4 receptor antagonist with a Ki of 1.3 nM, less potent to EP3, FP, and TP receptors with Ki of 30 nM, 790 nM, and 2400 nM, respectively. |
|
|
S3738 |
Travoprost
|
Travoprost (Travoprostum) is a PGF2a analog that was launched as an ophthalmic solution administered topically for the treatment of elevated intraocular hypertension as a result of open-angle glaucoma, a common optic neuropathy, and a leading cause of blindness. It can act as an agonist of prostaglandin F receptor. |
|
|
S5056 |
Dinoprost tromethamine
|
Dinoprost Tromethamine (Dinolytic, PGF2-alpha tham, Zinoprost, Prostin F2 alpha, Dinoprost Trometamol) is a synthetic analogue of the naturally occurring prostaglandin F2 alpha, which stimulates myometrial activity, relaxes the cervix, inhibits corpus luteal steroidogenesis, and induces luteolysis by direct action on the corpus luteum. |
|
|
E2146New |
Iloprost
|
Iloprost(Ciloprost, ZK 36374, Ventavis) is a prostacyclin (PGI2) analogue and is a potent agonist of the prostacyclin IP receptor and the prostaglandin E2 (PGE2) receptor subtype EP1. It exhibits high binding affinity for EP1 and IP receptors with Ki values of 1.1 nM and 3.9 nM, respectively. |
|
|
S2072 |
Seratrodast(AA-2414)
|
Seratrodast (AA-2414, ABT-001) is a potent and selective thromboxane A2 receptor (TP) antagonist which is used primarily in the treatment of asthma and used as anti-inflammatory agent.
|
|
|
S4415 |
Misoprostol
|
Misoprostol(SC29333) is a synthetic prostaglandin E1 (PGE1) analog that is used to prevent gastric ulcers, to treat missed miscarriage, to induce labor, and to induce abortion. |
|
|
S7211 |
PF-04418948
|
PF-04418948 is a potent and selective prostaglandin EP₂ receptor antagonist with IC50 of 16 nM. Phase 1.
|
- Int J Mol Sci, 2023, 24(13)10881
- Cancer Res Commun, 2023, 3(8):1486-1500
- Cancer Res Commun, 2023, 3(8):1486-1500
|
|
S6793 |
TG4-155
|
TG4-155 is a potent and selective Prostaglandin Receptor EP2(PTGER2) antagonist with Ki value of 9.9 nM. |
- Elife, 2023, 12e81438
- Elife, 2023, 12e81438
- bioRxiv, 2021, 10.1101/2021.08.27.457936
|
|
S6694 |
Grapiprant (CJ-023,423)
|
Grapiprant (CJ-023,423, AT-001, AAT-007, RQ-00000007, CJ-23423) is a novel selective EP4 Prostaglandin Receptor inhibitor with Ki of 20 nM and 13 nM for rat EP4 receptor and human EP4 receptor, respectively. |
- Bone Res, 2022, 10(1):27
|
|
S0495 |
BI-671800
|
BI-671800 (AP-761, Cmpd A) is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2) with IC50 of 4.5 nM and 3.7 nM for PGD2 binding to human CRTH2 and murine CRTH2, respectively. BI-671800 is associated with a small improvement in FEV1 in symptomatic controller-naïve asthma patients, and in patients on ICS. |
|
|
S5753 |
Setipiprant (ACT-129968)
|
Setipiprant (ACT-129968, KYTH-105) is a selective, orally available antagonist of the prostaglandin D2 receptor 2 (DP2) that that has been shown to have greater specificity for DP2 (CRTH2) than for DP1. |
|
|
S0305 |
RO1138452
|
RO1138452 (CAY10441) is a potent and selective antagonist of IP (prostacyclin, PGI2) receptor with pKi of 9.3 and 8.7 in human platelets and a recombinant IP receptor system, respectively. |
|
|
S5286 |
Ramatroban
|
Ramatroban (BAY u 3405) is a thromboxane A2(TxA2) receptor antagonist with Ki value of 10 to 13 nM. It also antagonizes a newly identified PGD2 receptor, CRTh2 expressed on the inflammatory cells. |
|
|
E2873 |
Laropiprant
|
Laropiprant is a potent and selective prostaglandin D2 (DP) receptor antagonist with a Ki value of 0.57 nM.
|
|
|
S0099 |
Asapiprant
|
Asapiprant(S-555739) is a potent and selective DP1 receptor antagonist with a Ki of 0.44 nM, which has potential as a novel therapy for allergic airway diseases. |
|
|
E0612 |
MF-766
|
MF-766 is a highly potent, selective and orally active EP4 antagonist with a Ki of 0.23 nM. |
|
|
E0809 |
Timapiprant Sodium
|
Timapiprant sodium (OC000459 sodium), a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist, potently displaces [3H]PGD2 from human recombinant DP2, rat recombinant DP2, and human native DP2 with Ki values of 13, 3 and 4 nM, respectively. |
|
|
E2986 |
ONO-AE3-208
|
ONO-AE3-208(AE 3-208) is a selective and orally active EP4 receptor antagonist with a Ki of 1.3 nM, less potent to EP3, FP, and TP receptors with Ki of 30 nM, 790 nM, and 2400 nM, respectively. |
|
|
S2072 |
Seratrodast(AA-2414)
|
Seratrodast (AA-2414, ABT-001) is a potent and selective thromboxane A2 receptor (TP) antagonist which is used primarily in the treatment of asthma and used as anti-inflammatory agent.
|
|
|
S3003 |
Prostaglandin E2 (PGE2)
|
Prostaglandin E2 (PGE2, Dinoprostone) plays important effects in labour (softens cervix and causes uterine contraction) and also stimulates osteoblasts to release factors that stimulate bone resorption by osteoclasts.
|
- J Exp Clin Cancer Res, 2024, 43(1):277
- Front Pharmacol, 2024, 15:1372109
- bioRxiv, 2024, 2024.07.12.603155
|
|
S1407 |
Bimatoprost
|
Bimatoprost(AGN 192024) is a prostaglandin analog used topically (as eye drops) to control the progression of glaucoma and in the management of ocular hypertension. |
- PLoS Pathog, 2020, 16;16(3):e1008341
- Invest Ophthalmol Vis Sci, 2018, 59(15):5912-5923
|
|
S3726 |
Selexipag
|
Selexipag (NS-304, ACT-293987) is an orally active, first-in-class, selective prostacyclin IP receptor agonist with Ki value of 260 nM for human IP, whereas Ki values > 10,000 nM are measured at the other human G-protein-coupled prostanoid receptors (EP1-4, DP, FP and TP). |
- J Immunother Cancer, 2024, 12(11)e009805
- Biol Pharm Bull, 2022, 10.1248/bpb.b21-01057
- Front Med (Lausanne), 2021, 8:742436
|
|
S4851 |
Tafluprost
|
Tafluprost (AFP-168,MK2452) is a novel prostaglandin analog with a high affinity for the fluoroprostaglandin (FP) receptor PGF2α. A prostanoid selective FP receptor agonist. |
|
|
S9327 |
Carboprost
|
Carboprost is a synthetic prostaglandin analogue of PGF2α with oxytocic properties. |
|
|
S0325 |
Treprostinil sodium
|
Treprostinil sodium is a potent agonist of DP1, EP2 and IP receptors with Ki 4.4 nM, 3.6 nM and 32 nM, respectively. |
|
|
E4846New |
Treprostinil
|
Treprostinil is a potent agonist of DP1 and EP2 with EC50 of 0.6 nM and 6.2 nM for DP1 and EP2 receptors, respectively. It is a vasodilator used to treat pulmonary arterial hypertension and improves mitochondrial impairment in vitro. |
|
|
S0111 |
Taprenepag
|
Taprenepag(CP-544326) is a potent and selective prostaglandin EP2 agonist with IC50s of 10 and 15 nM for human and rat EP2, respectively. |
|
|
E0053 |
Evatanepag
|
Evatanepag (CP-533536 free acid) is a potent and selective EP2 receptor agonist with an IC50 of 50 nM for rEP2.
|
|
|
S5819 |
MRE-269 (ACT-333679)
|
MRE-269 (ACT-333679) is a prostaglandin I2 (IP) receptor agonist with a binding affinity for the human IP receptor that is 130-fold greater than that for other human prostanoid receptor. |
|
|
S3738 |
Travoprost
|
Travoprost (Travoprostum) is a PGF2a analog that was launched as an ophthalmic solution administered topically for the treatment of elevated intraocular hypertension as a result of open-angle glaucoma, a common optic neuropathy, and a leading cause of blindness. It can act as an agonist of prostaglandin F receptor. |
|
|
S5056 |
Dinoprost tromethamine
|
Dinoprost Tromethamine (Dinolytic, PGF2-alpha tham, Zinoprost, Prostin F2 alpha, Dinoprost Trometamol) is a synthetic analogue of the naturally occurring prostaglandin F2 alpha, which stimulates myometrial activity, relaxes the cervix, inhibits corpus luteal steroidogenesis, and induces luteolysis by direct action on the corpus luteum. |
|
|
E2146New |
Iloprost
|
Iloprost(Ciloprost, ZK 36374, Ventavis) is a prostacyclin (PGI2) analogue and is a potent agonist of the prostacyclin IP receptor and the prostaglandin E2 (PGE2) receptor subtype EP1. It exhibits high binding affinity for EP1 and IP receptors with Ki values of 1.1 nM and 3.9 nM, respectively. |
|
|
S4415 |
Misoprostol
|
Misoprostol(SC29333) is a synthetic prostaglandin E1 (PGE1) analog that is used to prevent gastric ulcers, to treat missed miscarriage, to induce labor, and to induce abortion. |
|
|