Prostaglandin Receptor Antagonist

ONO-8711 dicyclohexylamine is a selective and orally active EP1 competitive antagonist with K_i value of 0.6 nM and 1.7 nM for human and mouse EP1 respectively. ONO-8711 dicyclohexylamine effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer.

TG6-10-1 is an EP2 antagonist, shows low-nanomolar antagonist activity against only EP2, >300-fold selectivity over human EP3, EP4, and IP receptors, 100-fold selectivity over EP1 receptors.

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

AL-8810 is a potent and selective antagonist of the PGF _2α receptor (FP receptor). AL-8810 is an activator of MAPK and ERK1/2. The K_i of the FP receptor of mouse 3T3 cells and rat A7r5 cells are 0.2±0.06 μM and 0.4±0.1 μM, respectively. AL-8810 can be used in the study of elevated intraocular pressure (OHT) and primary open-angle glaucoma (POAG).

SQ 29548 is a selective thromboxane-prostanoid (TP) receptor antagonist.

Vidupiprant (AMG 853) is a phenylacetic acid derivative. Vidupiprant is a potent and orally active CRTH2 (DP2) and prostanoid D receptor (DP or DP1) dual antagonist with IC₅₀s of 3 nM and 4 nM in buffer, and 8 nM and 35 nM in human plasma, respectively. Vidupiprant has the potential for asthma treatment.

TG8-260 is a second-generation EP2 antagonist developed to alleviate the pathology of central nervous system and peripheral diseases driven by inflammation. TG8-260 can reduce neuroinflammation and gliosis in the hippocampus of rats after pilocarpine-induced persistent epileptic status. Pharmacokinetic data of TG8-260 showed that its plasma half-life was 2.14 hours and its oral bioavailability was 77.3%. TG8-260 is also a potent inhibitor of CYP450 and shows antagonistic activity in inhibiting EP2 receptor-mediated inflammatory gene expression in BV2-hEP2 microglia, which is suitable for studying anti-inflammatory pathways in animal models of peripheral inflammatory diseases.

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

EP2 receptor antagonist-3 is a selective EP2 receptor antagonist (IC₅₀: 8 nM in hEP2 SPA assay, 50 nM in hEP2 cAMP assay). EP2 receptor antagonist-3 increases the macrophage-mediated clearance of Amyloid-β plaques. EP2 receptor antagonist-3 can be used for the study of alzheimer’s diseases.

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.

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.

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.

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.

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.

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.

ARRY-502 is an orally active, potent and selective CRTh2 antagonist. ARRY-502 blocks PGD2-mediated Th2 inflammation (e.g., eosinophil activation, airway hyperresponsiveness). ARRY-502 is promising for research of Th2-related asthma.

ACT-774312 is a potent and selective CRTH2 antagonist with an IC₅₀ of 4 nM. ACT-774312 blocks the activity and internalization of the CRTH2 receptor, and inhibits PGD₂-induced morphological changes in eosinophils. ACT-774312 can be used in the research of nasal polyps and type 2 inflammatory diseases.