Prostaglandin Receptor

Inhibitory Selectivity

Isoform-specific Inhibitors

Prostaglandin Receptor Products

New Prostaglandin Receptor Products
Catalog No. Information Product Use Citations Product Validations
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.

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.

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.

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.

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.

E0809New

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.

S6694New

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.

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.

S6793

TG4-155

TG4-155 is a potent and selective Prostaglandin Receptor EP2(PTGER2) antagonist with Ki value of 9.9 nM.

S0010

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.

S0325

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.

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.

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.

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.

Catalog No. Information Product Use Citations Product Validations
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.

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.

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.

Catalog No. Information Product Use Citations Product Validations
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.

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.

E0809New

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.

S6694New

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.

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.

S6793

TG4-155

TG4-155 is a potent and selective Prostaglandin Receptor EP2(PTGER2) antagonist with Ki value of 9.9 nM.

Catalog No. Information Product Use Citations Product Validations
S0010

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.

S0325

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.

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.

Catalog No. Information Product Use Citations Product Validations
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.

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.