Prostaglandin Receptor Antagonist

EP2 receptor antagonist-1 (compound 1) is a potent, reversible, and agonist dependent allosteric prostaglandin EP2 receptor antagonist. EP2 receptor antagonist-1 shows anti-inflammatory effects.

BI-671800 is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2), with IC₅₀ values of 4.5 nM and 3.7 nM for PGD2 binding to CRTH2 in hCRTH2 and mCRTH2 transfected cells, respectively. BI-671800 has potential for the treatment of poorly controlled asthma.

AAT-008 is a potent, selective, and orally active prostaglandin EP4 receptor antagonist with K_is of 0.97 and 6.1 nM for recombinant human EP4 and recombinant rat EP4, respectively. AAT-008 exerts tumor growth delay in mice bearing CT26WT colon tumors when combined with radiotherapy. AAT-008 can be used for the study of acute and chronic inflammatory pain and cancer .

EP4-IN-1 is a potent prostanoid EP4 receptor inhibitor. EP4-IN-1 is extracted from patent WO2023025270 (example 1), and exhibits prospect in tumor immunity and anti-inflammatory analgesia research.

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

L 888607 Racemate is a selective prostaglandin D₂ receptor subtype 1 (DP1) antagonist, with K_is of 132 nM and 17 nM for DP1 and thromboxane A2 receptor (TP), respectively.

BAY 73-1449 is a selective antagonist of prostacyclin receptor (IP), with high potency (IC₅₀ of less than 0.1 nM) in cAMP assays in Human HEL cells and rat DRG. BAY 73-1449 can be used in the research of lowering blood pressure.

SC-19220 is a prostaglandin E₂ receptor EP1 antagonist. SC-19220 blocks functional EP1 receptor activation, and RANK/RANKL signaling pathway. SC-19220 inhibits osteoclast formation and bone resorption by pre-existing osteoclasts. SC-19220 can be used for the research of osteoporotic disorders, inflammatory bone resorption.

EP4 receptor antagonist 2 (Compound 8) is a tricyclic spiro-based EP₄ receptor antagonist with microsomal stability.

Daltroban (BM-13505) is a selective and specific thromboxane A2 (TXA2) receptor antagonist. Daltroban increase intracellular calcium in vascular smooth muscle cells. Daltroban shows protective effect in reperfusion injury.

LAS191859 is an orally active, potent and selective CRTh2 antagonist with an IC₅₀ of 9.58 nM against human CRTh2. LAS191859 can be used for the research of chronic asthma.

RO3244794 is a potent and selective IP (prostacyclin) receptor antagonist, with a pK_i of 7.7 and 6.9 in human platelet and recombinant IP receptor system, respectively. RO3244794 exhibits analgesic and anti-inflammatory potential.

Setipiprant (ACT-129968) is an orally active and selective CRTH2 antagonist. Setipiprant interacts with hCRTH2 receptor with an IC₅₀ value of 6 nM. Setipiprant inhibits prostanoid receptors hDP₁ and hEP₂ with IC₅₀ values of 1290 and 2600 nM, respectively. Setipiprant can be used for the research of asthma and rhinitis.

Terutroban (S-18886) sodium is a selective and orally active thromboxane-prostaglandin (TP) receptor antagonist with an IC₅₀ of 16.4 nM. Terutroban sodium inhibits TXA2 and prostaglandin endoperoxide receptors. Terutroban sodium is a potent antithrombotic agent and possesses anti-atherosclerotic and anti-vasoconstrictor properties.

CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective prostaglandin D2 receptor CRTH2 antagonist, with a K_i of 0.6 nM for hCRTH2, selective over human thromboxane A2 receptor TP (K_i, >10000 nM) or PGD2 receptor DP (K_i, 1200 nM). CAY10471 Racemate also has effect on mouse and rat orthologs of CRTH2.

MK-7246 is a potent and selective CRTH2 antagonist with a K_i of 2.5±0.5 nM.

HTL0039732 is an orally active antagonist of the prostaglandin EP4 receptor (Prostaglandin E2 Receptor EP4). HTL0039732 reverses PGE₂-induced differentiation toward M2-like macrophages. HTL0039732 exhibits efficacy in syngeneic tumor models and acts synergistically with PD-1/PD-L1 pathway blockers. HTL0039732 can be used for the research of advanced solid tumors.

Ifetroban (BMS-180291) is an orally active antagonist of thromboxane A2 (TXA2) or prostaglandin H2 (PGH2) receptor. Ifetroban shows antiplatelet activity, and inhibits tumor cell migration without affecting cell proliferation. Ifetroban can be used for myocardial ischemia, hypertension, stroke, thrombosis, cardiomyopathy research.

BAY-1316957 is a potent, selective and orally active prostaglandin E2 receptor subtype 4 (EP4-R) antagonist with an IC₅₀ of 15.3 nM for human EP4-R. BAY-1316957 has excellent agent metabolism and pharmacokinetics properties, and can be used for endometriosis research.

EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4 with an IC₅₀ value of 1.1 nM. EP4 receptor antagonist 7 inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC₅₀ value of 0.9 nM. EP4 receptor antagonist 7 decreases PGE2-induced expression of mRNA encoding IL-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C) motif ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase-1 (Arg1), in RAW 264.7 macrophages. EP4 receptor antagonist 7 combined with an anti-PD-1 antibody inhibits tumor growth and increases infiltration of CD⁸⁺ T cells into tumors in a CT26 murine colon cancer model.