A selective PAR4 antagonist (IC50 = 0.56 nM); selective for PAR4 over PAR1

BMS 986120 – 10 mg

Brand:
Cayman
CAS:
1478712-37-6
Storage:
-20
UN-No:
Non-Hazardous - /

BMS 986120 is an orally bioavailable, selective, and reversible antagonist of proteinase-activated receptor 4 (PAR4; IC50 = 0.56 nM to inhibit calcium mobilization induced by PAR4 agonist peptide (PAR4-AP) in HEK293 cells).{36234} It is selective for PAR4 over PAR1, PAR2, and a panel of purified proteases, including thrombin. It inhibits platelet aggregation in vitro in human platelet-rich plasma (IC50 = 7.3 nM). BMS 986120 (0.2-1 mg/kg) decreases platelet aggregation induced by PAR4-AP ex vivo in a dose-dependent manner, but does not increase clotting times. In vivo, BMS 986120 (1 mg/kg) prevents vascular occlusion and reduces thrombus formation by 82% in cynomolgus monkeys.  

 

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SKU: 23497 - 10 mg Category:

Description

A selective PAR4 antagonist (IC50 = 0.56 nM); selective for PAR4 over PAR1, PAR2, and a panel of purified proteases; inhibits platelet aggregation in vitro in human platelet-rich plasma (IC50 = 7.3 nM); decreases platelet aggregation ex vivo at a dose of 0.2-1 mg/kg; prevents vascular occlusion and reduces thrombus formation by 82% in cynomolgus monkeys

Formal name: 2-methoxy-6-[6-methoxy-4-[[5-methyl-2-(4-morpholinyl)-4-thiazolyl]methoxy]-2-benzofuranyl]-imidazo[2,1-b]-1,3,4-thiadiazole

Synonyms: 

Molecular weight: 513.6

CAS: 1478712-37-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Blood|Coagulation & Hemostasis||Research Area|Cardiovascular System|Blood|Thrombosis

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