Pricing updated 2019-05-23. Prices are subject to change without notice.
Vorapaxar is an orally bioavailable competitive antagonist of the proteinase-activated receptor (PAR1; Ki = 8.1 nM), also known as the thrombin receptor.1 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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Chackalamannil, S., Wang, Y., Greenlee, W.J., et al. Discovery of a novel, orally active himbacine-