Vorapaxar sulfate |
Catalog No.GC64347 |
Le sulfate de vorapaxar (SCH 530348 sulfate), un agent antiplaquettaire, est un antagoniste sélectif, actif par voie orale et compétitif du récepteur activé par la protéase du récepteur de la thrombine (PAR-1) (Ki = 8,1 nM).
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Cas No.: 705260-08-8
Sample solution is provided at 25 µL, 10mM.
Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner[1].
Vorapaxar sulfate (SCH 530348 sulfate) shows potent inhibition of thrombin-induced platelet aggregation with an IC50 of 47 nM and haTRAP-induced platelet aggregation with an IC50 of 25 nM. Vorapaxar sulfate (SCH 530348 sulfate) inhibits thrombininduced calcium transient in human coronary artery smooth muscle cells (HCASMC) with a Ki of 1.1 nM. It also inhibits thrombin-stimulated thymidine incorporation in HCASMC with a Ki of 13 nM[1].
[1]. Khoufache K, et al. PAR1 contributes to influenza A virus pathogenicity in mice. J Clin Invest. 2013 Jan;123(1):206-14.
[2]. Kehinde O, et al. Vorapaxar: A novel agent to be considered in the secondary prevention of myocardial infarction. J Pharm Bioallied Sci. 2016 Apr-Jun;8(2):98-105.
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