Prostaglandin Receptor
Inhibitory Selectivity
Prostaglandin Receptor Products
Catalog No. | Information | Product Use Citations | Product Validations |
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S2496 |
OzagrelOzagrel (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. |
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S2067 |
Ozagrel HClOzagrel HCl (OKY-046) is a selective |
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S3304New |
StylopineStylopine ((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. |
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S0141New |
NQ301NQ301 (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. |
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S5252 |
Ozagrel sodiumOzagrel sodium (KCT-0809, Cataclot, Xanbo) is a thromboxane A2 synthase (CYP5) inhibitor with neuroprotective properties. |
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S3816 |
DehydroevodiamineDehydroevodiamine (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. |
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S5594 |
α-Terpineolα-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. |
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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. |
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S6850New |
NE 52-QQ57NE 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). |
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S0495New |
BI-671800BI-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. |
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S0305New |
RO1138452RO1138452 (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. |
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S6793New |
TG4-155TG4-155 is a potent and selective Prostaglandin Receptor EP2(PTGER2) antagonist with Ki value of 9.9 nM. |
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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. |
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S7211 |
PF-04418948PF-04418948 is a potent and selective prostaglandin EP₂ receptor antagonist with IC50 of 16 nM. Phase 1. |
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S5286 |
RamatrobanRamatroban (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. |
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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. |
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S1407 |
BimatoprostBimatoprost is a prostaglandin analog used topically (as eye drops) to control the progression of glaucoma and in the management of ocular hypertension. |
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S1508 |
AlprostadilAlprostadil (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. |
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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. |
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S0325New |
Treprostinil sodiumTreprostinil 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. |
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S0010New |
RalinepagRalinepag (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. |
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S4851 |
TafluprostTafluprost (AFP-168) is a novel prostaglandin analog with a high affinity for the fluoroprostaglandin (FP) receptor PGF2α. A prostanoid selective FP receptor agonist. |
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S9327 |
CarboprostCarboprost is a synthetic prostaglandin analogue of PGF2α with oxytocic properties. |
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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. |
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S3726 |
SelexipagSelexipag (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). |
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S3738 |
TravoprostTravoprost (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 tromethamineDinoprost 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. |
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S4415 |
MisoprostolMisoprostol(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. |
||
S3346New |
1-Methylnicotinamide chloride1-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. |
||
S0541New |
Dazoxiben hydrochlorideDazoxiben 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 |
EthamsylateEthamsylate (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 |
OzagrelOzagrel (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 HClOzagrel HCl (OKY-046) is a selective |
||
S3304New |
StylopineStylopine ((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. |
||
S0141New |
NQ301NQ301 (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 sodiumOzagrel sodium (KCT-0809, Cataclot, Xanbo) is a thromboxane A2 synthase (CYP5) inhibitor with neuroprotective properties. |
||
S3816 |
DehydroevodiamineDehydroevodiamine (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-Terpineolα-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 | Product Validations |
---|---|---|---|
S6850New |
NE 52-QQ57NE 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). |
||
S0495New |
BI-671800BI-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. |
||
S0305New |
RO1138452RO1138452 (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. |
||
S6793New |
TG4-155TG4-155 is a potent and selective Prostaglandin Receptor EP2(PTGER2) antagonist with Ki 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-04418948PF-04418948 is a potent and selective prostaglandin EP₂ receptor antagonist with IC50 of 16 nM. Phase 1. |
||
S5286 |
RamatrobanRamatroban (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 | Product Validations |
---|---|---|---|
S1407 |
BimatoprostBimatoprost is a prostaglandin analog used topically (as eye drops) to control the progression of glaucoma and in the management of ocular hypertension. |
||
S1508 |
AlprostadilAlprostadil (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. |
||
S0325New |
Treprostinil sodiumTreprostinil 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. |
||
S0010New |
RalinepagRalinepag (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 |
TafluprostTafluprost (AFP-168) is a novel prostaglandin analog with a high affinity for the fluoroprostaglandin (FP) receptor PGF2α. A prostanoid selective FP receptor agonist. |
||
S9327 |
CarboprostCarboprost 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 |
SelexipagSelexipag (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 |
TravoprostTravoprost (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 tromethamineDinoprost 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 |
MisoprostolMisoprostol(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 |
---|---|---|---|
S3346New |
1-Methylnicotinamide chloride1-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. |
||
S0541New |
Dazoxiben hydrochlorideDazoxiben 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 |
EthamsylateEthamsylate (Etamsylate) is a haemostatic drug, which inhibits biosynthesis and action of prostaglandins, and increases capillary endothelial resistance as and platelet adhesion. |