Prostaglandin Receptor

Inhibitory Selectivity

Prostaglandin Receptor Products

All (31) Prostaglandin Receptor Inhibitors (8) Prostaglandin Receptor Antagonists (8) Prostaglandin Receptor Agonists (12) Prostaglandin Receptor Modulators (2)

Catalog No.	Information	Product Use Citations
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.
S3304^New	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.
S0141^New	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.
S5252	Ozagrel sodium Ozagrel sodium (KCT-0809, Cataclot, Xanbo) is a thromboxane A2 synthase (CYP5) inhibitor with neuroprotective properties.
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.
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.
S6649	E7046 (ER-886406) E7046 (ER-886406) is a selective inhibitor of the prostaglandin E₂ (PGE₂) receptor EP4 with IC50 of 13.5 nM and Ki of 23.14 nM.
S6850^New	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).
S0495^New	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.
S0305^New	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.
S6793^New	TG4-155 TG4-155 is a potent and selective Prostaglandin Receptor EP2(PTGER2) antagonist with K_i value of 9.9 nM.
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.
S7211	PF-04418948 PF-04418948 is a potent and selective prostaglandin EP₂ receptor antagonist with IC50 of 16 nM. Phase 1.	Nat Commun, 2019, 10(1):1888 Arterioscler Thromb Vasc Biol, 2018, 38(5):1115-1124
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.
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.
S1407	Bimatoprost Bimatoprost 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
S1508	Alprostadil Alprostadil (Prostaglandin-E1) is used as a drug in the treatment of erectile dysfunction and has vasodilatory properties. It is a Prostaglandin Analog and Prostaglandin E1 Agonist.
S3003	Prostaglandin E2 (PGE2) Prostaglandin E2 (PGE2, Dinoprostone) palys important effects in labour (softens cervix and causes uterine contraction) and also stimulates osteoblasts to release factors that stimulate bone resorption by osteoclasts.	Nat Commun, 2020, 11(1):6339 Am J Cancer Res, 2020, 10(9):2813-2831 Acta Pharmacol Sin, 2020, 10.1038/s41401-020-00504-4
S0325^New	Treprostinil sodium Treprostinil sodium (UT-15, Remodulin, Orenitram, Tyvaso, Trevyent) is a potent agonist of DP1, EP2 and IP receptors with Ki 4.4 nM, 3.6 nM and 32 nM, respectively.
S0010^New	Ralinepag Ralinepag (APD811) is a potent, orally bioavailable and non-prostanoid prostacyclin (IP) receptor agonist with EC50 of 8.5 nM, 530 nM and 850 nM for human IP receptor, rat IP receptor and human DP1 receptor, respectively.
S4851	Tafluprost Tafluprost (AFP-168) 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.
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.
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).
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.
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.
S3346^New	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.
S0541^New	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.
S4152	Ethamsylate Ethamsylate (Etamsylate) is a haemostatic drug, which inhibits biosynthesis and action of prostaglandins, and increases capillary endothelial resistance as and platelet adhesion.

Catalog No.	Information	Product Use Citations	Product Validations
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.
S3304^New	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.
S0141^New	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.
S5252	Ozagrel sodium Ozagrel sodium (KCT-0809, Cataclot, Xanbo) is a thromboxane A2 synthase (CYP5) inhibitor with neuroprotective properties.
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.
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.
S6649	E7046 (ER-886406) E7046 (ER-886406) is a selective inhibitor of the prostaglandin E₂ (PGE₂) receptor EP4 with IC50 of 13.5 nM and Ki of 23.14 nM.

Catalog No.	Information	Product Use Citations
S6850^New	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).
S0495^New	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.
S0305^New	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.
S6793^New	TG4-155 TG4-155 is a potent and selective Prostaglandin Receptor EP2(PTGER2) antagonist with K_i value of 9.9 nM.
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.
S7211	PF-04418948 PF-04418948 is a potent and selective prostaglandin EP₂ receptor antagonist with IC50 of 16 nM. Phase 1.	Nat Commun, 2019, 10(1):1888 Arterioscler Thromb Vasc Biol, 2018, 38(5):1115-1124
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.
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.

Catalog No.	Information	Product Use Citations
S1407	Bimatoprost Bimatoprost 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
S1508	Alprostadil Alprostadil (Prostaglandin-E1) is used as a drug in the treatment of erectile dysfunction and has vasodilatory properties. It is a Prostaglandin Analog and Prostaglandin E1 Agonist.
S3003	Prostaglandin E2 (PGE2) Prostaglandin E2 (PGE2, Dinoprostone) palys important effects in labour (softens cervix and causes uterine contraction) and also stimulates osteoblasts to release factors that stimulate bone resorption by osteoclasts.	Nat Commun, 2020, 11(1):6339 Am J Cancer Res, 2020, 10(9):2813-2831 Acta Pharmacol Sin, 2020, 10.1038/s41401-020-00504-4
S0325^New	Treprostinil sodium Treprostinil sodium (UT-15, Remodulin, Orenitram, Tyvaso, Trevyent) is a potent agonist of DP1, EP2 and IP receptors with Ki 4.4 nM, 3.6 nM and 32 nM, respectively.
S0010^New	Ralinepag Ralinepag (APD811) is a potent, orally bioavailable and non-prostanoid prostacyclin (IP) receptor agonist with EC50 of 8.5 nM, 530 nM and 850 nM for human IP receptor, rat IP receptor and human DP1 receptor, respectively.
S4851	Tafluprost Tafluprost (AFP-168) 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.
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.
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).
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.
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.

Catalog No.	Information	Product Use Citations	Product Validations
S3346^New	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.
S0541^New	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.

Catalog No.

Information

Product Use Citations

Product Validations

S3346^New

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.

S0541^New

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.

Catalog No.	Information	Product Use Citations	Product Validations
S4152	Ethamsylate Ethamsylate (Etamsylate) is a haemostatic drug, which inhibits biosynthesis and action of prostaglandins, and increases capillary endothelial resistance as and platelet adhesion.

Catalog No.

Information

Product Use Citations

Product Validations

S4152

Ethamsylate

Ethamsylate (Etamsylate) is a haemostatic drug, which inhibits biosynthesis and action of prostaglandins, and increases capillary endothelial resistance as and platelet adhesion.

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Prostaglandin Receptor Products