Prostaglandin Receptor Antagonist

EP2 receptor antagonist-2 (CID891729) is an antagonist of EP2 receptor. EP2 receptor antagonist-2 inhibits the EP2 receptor activation induced by PGE2. EP2 receptor antagonist-2 also suppresses lactate dehydrogenase (LDH) release induced by N-methyl-D-aspartate (NMDA).

AS604872 is an orally active, potent and selective prostaglandin F2α receptor (FP) antagonist with a K_i of 35 nM in humans, 158 nM in rats and 323 nM in mice. AS604872 inhibits contractions and delays labour.

PGD2-IN-1 is an antagonist of DP extracted from patent WO 2006044732 A2, example 15 (d); has an IC₅₀ of 0.3 nM.

GSK-269984A is a Prostaglandin E2 Receptor 1 (EP1) antagonist with a pIC₅₀ of 7.9.

Pexopiprant is an oral antagonist of the prostaglandin D2 receptor 2 (DP2),K_i ＜ 100nM. Pexopiprant can be used in studies of asthma.

AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC₅₀s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively.

EP1-antagonist-1 (Compound 27) is an EP1 antagonist with a pK_i (FLIPR) of 9.31 and a pIC₅₀ (binding) of 9.88. EP1-antagonist-1 can be used for the study of PGE2-mediated pain.

KP496 is a selective, dual antagonist for Leukotriene D4 receptor and Thromboxane A2 receptor.

BGC-20-1531 (PGN 1531) free base is a potent and selective prostanoid EP₄ receptor antagonist, with a pK_B of 7.6. BGC-20-1531 free base has the potential for the research of migraine headache.

AMX12006 is a potent, selective and orally active EP4 antagonist with an IC₅₀ value of 4.3 nM. AMX12006 shows cytotoxic and antitumor activity.

MK-2894 sodium salt is a potent, selective, orally active and high affinity (K_i=0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) (IC₅₀=2.5 nM). MK-2894 sodium salt possesses potent anti-inflammatory activity in animal models of pain/inflammation and can be used for the research of arthritis.

AMG-009 is a potent antagonist of prostaglandin D2, with IC₅₀ of 3 nM and 12 nM for CRTH2 and DP receptors, respectively.

TP receptor antagonist-3 (compound 51280) is a potent thromboxane A2 prostanoid (TP) receptor with an IC₅₀ of 15.7 nM against Human TP. TP receptor antagonist-3 can be used for alzheimer's disease, cardiovascular and respiratory diseases, and cancer research.

SC 51089 is a selective antagonist of prostaglandin E₂ EP1 receptor, with K_is of 1.3, 11.2, 17.5, and 61.1 μM for EP1, TP, EP3, and FP receptors, respectively. SC 51089 exhibits neuroprotective activity.

ONO-8711 is a potent and selective competitive antagonist of EP1 receptor (K_i = 0.6 and 1.7 nM for human and mouse EP1 respectively). ONO-8711 effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer.

RO1138452 (Standard) is the analytical standard of RO1138452. This product is intended for research and analytical applications. RO1138452 is a potent and selective IP (prostacyclin) receptor antagonist. RO1138452 displays high affinity for IP receptors. In human platelets, pKi is 9.3±0.1; in a recombinant IP receptor system, pKi is 8.7±0.06.

Seratrodast (Standard) is the analytical standard of Seratrodast. This product is intended for research and analytical applications. Seratrodast (AA 2414), an orally active antiasthmatic agent, is a thromboxane A2 receptor (TP) antagonist and ferroptosis inhibitor. Seratrodast reduces lipid ROS production, modulates the systemic xc-/GSH/GPX4 axis, and inhibits JNK phosphorylation and p53 expression. Seratrodast exhibits anti-asthmatic and anti-epileptic activity.

Sulotroban (SKF-95587; BM-13177) is a selective antagonist for thromboxane A2 receptor (TXA2 Receptor). Sulotroban exhibits inhibitory activity against carbocyclic thromboxane A2- and endoperoxide-induced vasoconstrictor. Sulotroban inhibits platelets aggregation.

TP-18 is a potent and orally active dual EP2/EP4 antagonist with IC₅₀ values of 9.5 nM (EP2) and 3.3 nM (EP4). TP-18 effectively depletes a highly immunosuppressive VSIG4high tumor-associated macrophage (TAM) subset and enhances cytotoxic CD8+ T cell-mediated colorectal cancer (CRC) tumor elimination. TP-18 dampens the expression of VSIG4 by blunting EP2/EP4-Gαs-PKA signaling. TP-18 enhances the sensitivity of anti-PD-1 therapy in CRC mouse models and in patient-derived tumor immune organoids. TP-18 can be used to study colorectal cancer.

BAY-6672, a chemical probe, is a potent and selective human Prostaglandin F (FP) receptor antagonist with an IC₅₀ value of 11 nM.