Prostaglandin Receptor Antagonist

Prostaglandin Receptor Antagonists (59):

Cat. No.	Product Name	Effect	Purity

HY-100449

AL-8810	Antagonist	99.00%
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).

HY-12182A

ONO-8711 dicyclohexylamine	Antagonist	99.30%
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.

HY-16978

TG6-10-1	Antagonist	99.92%
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.

HY-105218A

Ifetroban sodium	Antagonist	99.83%
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.

HY-14973

Vidupiprant	Antagonist	98.33%
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.

HY-133123

EP4 receptor antagonist 1	Antagonist	99.66%
EP4 receptor antagonist 1 is a highly potent and selective competitive prostanoid EP4 receptor antagonist for cancer immunotherapy. EP4 receptor antagonist 1 inhibits human and mouse EP4 receptor with IC₅₀s of 6.1 nM and 16.2 nM, respectively. IC₅₀s >10 μM for human EP1, EP2,and EP3 receptors.

HY-16991

Terutroban	Antagonist	99.84%
Terutroban (S-18886) is a selective and orally active thromboxane-prostaglandin (TP) receptor antagonist with an IC₅₀0 of 16.4 nM. Terutroban inhibits TXA2 and prostaglandin endoperoxide receptors. Terutroban is a potent antithrombotic agent and possesses antiatherosclerotic and antivasoconstrictor properties.

HY-108972

SQ 29548	Antagonist	≥99.0%
SQ 29548, a high affinity radioligand, is a selective thromboxane-prostanoid (TP) receptor antagonist.

HY-164049

TG8-260	Antagonist	98.25%
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.

HY-101430

PGD2-IN-1	Antagonist	98.24%
PGD2-IN-1 is an antagonist of DP extracted from patent WO 2006044732 A2, example 15 (d); has an IC₅₀ of 0.3 nM.

HY-123596

LAS191859	Antagonist
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.

HY-13213

AM211	Antagonist	98.79%
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.

HY-118388

AS604872	Antagonist
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.

HY-164580

RO3244794	Antagonist	99.64%
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.

HY-B0774R

Seratrodast (Standard)	Antagonist
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.

HY-12284

NVP-QAV680	Antagonist
NVP-QAV680 is a potent and selective CRTh2 receptor antagonist with low nanomolar (nM) functional potency to inhibit CRTh2-driven activation of human eosinophils and Th2 lymphocytes. NVP-QAV680 exhibits good oral bioavailability and demonstrates efficacy in CRTh2-dependent mechanisms and allergic disease models in rats.

HY-169859

EP4 receptor antagonist 7	Antagonist
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.

HY-115827

AH22921	Antagonist
AH22921 is an EP4 prostaglandin receptor antagonist with the activity of antagonizing the activation of adenylate cyclase by prostaglandins in CHO cells. AH22921 can shift the PGE2 concentration-response curve to the right in CHO cells. It is a non-competitive antagonist that is selective for EP4 receptors and has an antagonistic effect on EP4 receptors in CHO cells, but does not affect the PGE2 concentration-response curve in NPE cells containing EP2 receptors.

HY-111304

MF266-1	Antagonist
MF266-1 is a selective E prostanoid receptor 1 (EP1) antagonist with an K_i value of 3.8 nM. MF266-1 also has moderate selectivity for thromboxane A2 receptor (TP). MF266-1 is promising for research of arthritis.

HY-100570

KF15766	Antagonist
KF15766 (compd 34E) is an orally active TXA₂ and H₁ dual antagonist with K_is of 740 and 20 nM. KF15766 can be used for antiallergic research.

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