A PAR1 antagonist (Ki = 8.1 nM); selective for PAR1 over other PARs

Vorapaxar – 1 mg

Brand:
Cayman
CAS:
618385-01-6
Storage:
-20
UN-No:
De Minimis - 3077 / 9

Vorapaxar is an orally bioavailable competitive antagonist of the proteinase-activated receptor (PAR1; Ki = 8.1 nM), also known as the thrombin receptor.{37192} It is selective for PAR1 over other PARs, as well as a number of GPCRs, ion channels, and receptors. It inhibits platelet aggregation induced by thrombin (Item No. 13188) and haTRAP (IC50s = 47 and 25 nM, respectively). Vorapaxar (0.1 mg/kg, i.v.) completely inhibits platelet aggregation in cynomolgus monkeys ex vivo. Formulations containing vorapaxar are used in the prevention of thrombotic cardiovascular events.  

 

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SKU: 23119 - 1 mg Category:

Description

A PAR1 antagonist (Ki = 8.1 nM); selective for PAR1 over other PARs, as well as a number of GPCRs, ion channels, and receptors; inhibits thrombin- and haTRAP-induced platelet aggregation (IC50s = 47 and 25 nM, respectively); completely inhibits platelet aggregation in cynomolgus monkeys ex vivo when used at a dose of 0.1 mg/kg i.v.

Formal name: N-[(1R,3aR,4aR,6R,8aR,9S,9aS)-9-[(1E)-2-[5-(3-fluorophenyl)-2-pyridinyl]ethenyl]dodecahydro-1-methyl-3-oxonaphtho[2,3-c]furan-6-yl]-carbamic acid, ethyl ester

Synonyms: 

Molecular weight: 492.6

CAS: 618385-01-6

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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