Prostaglandin Receptor
Inhibitory Selectivity
Isoform-specific Inhibitors
Prostaglandin Receptor Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S6496 |
Genz-123346 free baseGenz-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. |
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| 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. |
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| S0141 |
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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| S0495 |
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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| S0305 |
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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| E0809New |
Timapiprant SodiumTimapiprant 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. |
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| 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. |
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| S0099 |
AsapiprantAsapiprant(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. |
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| S6793 |
TG4-155TG4-155 is a potent and selective Prostaglandin Receptor EP2(PTGER2) antagonist with Ki value of 9.9 nM. |
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| S0010 |
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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| S0325 |
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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| S0111 |
TaprenepagTaprenepag(CP-544326) is a potent and selective prostaglandin EP2 agonist with IC50s of 10 and 15 nM for human and rat EP2, respectively. |
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| E0053 |
EvatanepagEvatanepag (CP-533536 free acid) is a potent and selective EP2 receptor agonist with an IC50 of 50 nM for rEP2. |
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| S0541 |
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. |
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| S3346 |
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. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S6496 |
Genz-123346 free baseGenz-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 |
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. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S0495 |
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. |
||
| S0305 |
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. |
||
| E0809New |
Timapiprant SodiumTimapiprant 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 |
AsapiprantAsapiprant(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 |
TG4-155TG4-155 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 |
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. |
||
| S0325 |
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. |
||
| S0111 |
TaprenepagTaprenepag(CP-544326) is a potent and selective prostaglandin EP2 agonist with IC50s of 10 and 15 nM for human and rat EP2, respectively. |
||
| E0053 |
EvatanepagEvatanepag (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 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. |
||
| S3346 |
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. |
