P2Y1 antagonist 4

P2Y1 antagonist 4 is a selective P2Y1 receptor antagonist with excellent blood-brain barrier (BBB) penetration. P2Y1 antagonist 4 inhibits P2Y1 receptor-mediated cytosolic Ca2+ increase (IC50 = 1.95 μM) and platelet aggregation (IC50 = 3.24 μM) induced by ADP in rabbit washed platelets. P2Y1 antagonist 4 significantly upregulates the level of nuclear Nrf2 protein in H2O2-treated HT22 cells. P2Y1 antagonist 4 reduces myocardial infarct size in a mouse acute myocardial infarction (MI) model. P2Y1 antagonist 4 can be used for the study of ischemic stroke and myocardial infarction[1].

Product Specifications

UNSPSC

12352100

Target

Keap1-Nrf2; P2Y Receptor

Related Pathways

GPCR/G Protein; NF-κB

Field of Research

Neurological Disease; Cardiovascular Disease

Smiles

O=C1C2=C(C(F)F)N=C(C3=CC=CC(C#N)=C3)N2C=C(C4=CC=C(OC(F)(F)F)C=C4)N1

Molecular Formula

C21H11F5N4O2

Molecular Weight

446.33

References & Citations

[1]Zhang B, et al. Discovery of 1-Difluoromethyl-3- (3-cyanophenyl) -6-[4- (trifluoromethoxy) phenyl]imidazo[1,5-a]pyrazin-8- (7H) -one as a Potent P2Y1 Antagonist for the Treatment of Ischemic Stroke and Myocardial Infarction. J Med Chem. 2025 Aug 28;68 (16) :17990-18015.