Home GPCR & G Protein Prostaglandin Receptor

Prostaglandin Receptor Antagonists

Cat.No. Product Name Information Product Use Citations Product Validations
S7211 PF-04418948 PF-04418948 is a potent and selective prostaglandin EP₂ receptor antagonist with IC50 of 16 nM. Phase 1.
Arteriosclerosis, Thrombosis, and Vascular Biology, May 2018, 1115-1124
bioRxiv, February 10, 2026, nan
Cancer Research Communications, August 2023, 1486-1500
S6793 TG4-155 TG4-155 is a potent and selective Prostaglandin Receptor EP2(PTGER2) antagonist with Ki value of 9.9 nM.
Transl Neurodegener, 2025, 14(1):43
Elife, 2023, 12e81438
bioRxiv, 2021, 10.1101/2021.08.27.457936
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.
Life Sciences, May 27, 2024, 122746
Chinese Journal of Natural Medicines, February 2026, nan
Chinese Journal of Natural Medicines, February 04, 2026, nan
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 Research, March 09, 2022, 27
Bone Research, 2022, 27
Bone Res, 2022, 10(1):27
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.
Sci Adv, 2025, 11(29):eadv1492
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.
Molecules, 2025, 3772
Molecules, 2025, 30(18)3772
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. This compound 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.
E8082 Terutroban Terutroban (S-18886) is a potent and selective antagonist of thromboxane A2 prostanoid (TP) receptor with an IC50 of 16.4 nM. It exhibits antithrombotic, antivasoconstricting, and antiatherosclerotic properties and can represent a promising lead for the development of antithromboxane therapies.
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.
E7466 GW627368 GW627368 (GW627368X) is a potent and selective competitive antagonist of prostanoid EP4 receptors with additional human TP receptor affinity with pKi values of 7.0 and 6.8 for human prostanoid EP4 and TP receptors respectively. This compound may serve as a valuable tool for investigating the prostanoid EP4 receptor in various physiological and pathological contexts.
E2986 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.
E8198 TG6-10-1 TG6-10-1 is a selective, brain-penetrant antagonist of EP2 receptor with nanomolar potency. It reduces delayed mortality, neuroinflammation, and hippocampal neurodegeneration after status epilepticus (SE) in mice. This compound provides neuroprotection via anti-inflammatory mechanisms without direct anticonvulsant effects.