Prostaglandin Receptor

Prostaglandin Receptor製品

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  • Prostaglandin Receptor阻害剤 (8)
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  • Prostaglandin Receptor作動薬(12)
  • Prostaglandin Receptorモジュレータ(2)
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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.
Br J Cancer, 2023, 10.1038/s41416-023-02389-6
Br J Cancer, 2023, 129(8):1225-1237
JCI Insight, 2023, 8(6)e156057
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).
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.
E1477New 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.
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.
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.
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.
E2986New 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.
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.
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.
Br J Cancer, 2023, 10.1038/s41416-023-02389-6
Br J Cancer, 2023, 129(8):1225-1237
JCI Insight, 2023, 8(6)e156057
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).
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.
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.
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.
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
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.
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.
E1477New 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.
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.
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.
E2986New 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.
Br J Cancer, 2023, 10.1038/s41416-023-02389-6
Br J Cancer, 2023, 129(8):1225-1237
JCI Insight, 2023, 8(6)e156057
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).
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.
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.
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 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
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.
E1477New EP4-IN-1 EP4-IN-1 is a potent prostanoid EP4 receptor inhibitor. It exhibits prospects in tumor immunity and anti-inflammatory analgesia research.
E2986New 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.

Prostaglandin Receptor阻害剤の選択性比較

Tags: Prostaglandin Receptor agonist | Prostaglandin Receptor antagonist | Prostaglandin Receptor inhibitor