Prostaglandin Receptor Antagonist

TASP0376377 is a potent and selective CRTH2 antagonist (IC₅₀: 13 nM). TASP0376377 has binding affinity for CRTH2 (IC₅₀: 19 nM).

LCB 2853 sodium is a potent thromboxane A2/prostaglandin H2 (TXA2/PGH2) receptor antagonist. LCB 2853 sodium exhibits anti-aggregant and anti-vasospastic effects. LCB 2853 sodium can be used for the research of cardiovascular disease, such as hypertension.

EP3 antagonist 6 (compound 5) is a potent, orally and selective EP3 receptor antagonist, with an IC₅₀ of 1.9 nM. EP3 antagonist 6 can inhibits PGE2-induced (HY-101952) uterine contraction in pregnant rats.

ICI 192605 is a potent TXA2R (thromboxane A2 receptor) antagonist as cell signaling prostaglandin. ICI 192605 blocks contraction of isolated guinea pig trachea induced by U-46619.

AM432 (sodium) is a potent and selective antagonist of the DP₂ receptor (CRTH2). AM432 (sodium) exhibits excellent potency in a human whole blood eosinophil shape change assay with prolonged incubation. AM432 (sodium) also demonstrates excellent pharmacokinetics in dog and mouse models of inflammatory disease.

SQ-30741 is a thromboxane A2 receptor antagonist. SQ-30741 reduces vasoconstriction in a feline pulmonary vascular bed model. SQ-30741 increases relaxation of aortic endothelium and vascular smooth muscle in adult rats in a spontaneously hypertensive rat model. SQ-30741 can be used in research on cardiovascular diseases such as hypertension.

AZ-11665362 is a CRTh2 (DP2) receptor antagonist with an IC₅₀ of 2.6 nM. AZ-11665362 shows weak activity against aldose reductase, serotonin transporter, CYP 2C19, and CYP 2C9. AZ-11665362 lacks measurable inhibitory activity against COX-1 and COX-2. AZ-11665362 can be used for the research of asthma, and other inflammatory diseases.

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

AL-3138 (11-Deoxy-16-fluoro PGF2α) is a prostaglandin F2 alpha (PGF2alpha) analogue that antagonises FP prostaglandin receptor-mediated inositol phosphate production.

Terbogrel is an orally available thromboxane A2 receptor antagonist and a thromboxane A2 synthase inhibitor, with both IC₅₀s of about 10 nM.

Aligeron is a non-selective prostaglandin (PG) antagonist, and has vasodilatory properties.

CRTh2 antagonist 3 is a potent chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) antagonist. CRTh2 antagonist 3 enhances the activity of PDK1 toward a short peptide substrate, with an EC₅₀ of 2 μM and a K_d of 8.4 μM. CRTh2 antagonist 3 has the potential for cardiovascular inflammation.

Prostaglandin F2α dimethyl amide is an antagonist for Prostaglandin F2α (HY-12956), which blocks 50% contraction on gerbilMeriones unguiculatus colon induced by PGF2α at 3.2 μg/mL.

ONO-8130 is an orally active and selective prostanoid EP1 receptor antagonist. ONO-8130 blocks phosphorylation of ERK in the L6 spinal cord. ONO-8130 relieves bladder pain in mice with cyclophosphamide-induced cystitis. ONO-8130 can be used for interstitial cystitis research.

GW 848687X is a selective, orally active prostaglandin EP1 receptor antagonist for the inhibition of inflammatory pain. The oral bioavailability of GW 848687X was 54% in rats and 53% in dogs. GW 848687X has a half-life of 2 hours and has inhibitory potential for both acute and chronic pain.

L-670596 is an orally active and selective thrombsxane A2 receptor/prostaglandin receptor antagonist. L-670596 inhibits arachidonic acid (HY-109590) and U-44069 induced bronchoconstriction in the guinea pig. L-670596 also inhibits the aggregation of human platelet rich plasma induced by U-44069.

ER-819762 is an orally active, highly selective prostaglandin E₂ (PGE₂) EP₄ receptor antagonist with an EC₅₀ of 70 nM against human EP₄ receptor. ER-819762 can be used for rheumatoid arthritis research.

GSK-269984B is a potent EP1 antagonist. GSK-269984B has the potential for inflammatory pain research.

CAY10449 is an I prostanoid receptor antagonist. CAY10449 can reverse iloprost-induced TEER reduction. CAY10449 can also reverse the effect of ONO-1301 in mouse model. CAY10449 can be studied in research on athsma and allergic airway inflammation.

EP4 receptor antagonist 5 is a potent and selective prostanoid EP4 receptor antagonist that can reduce inflammation Freund’s adjuvant (CFA) model.