PeptideDB

Vorapaxar

CAS: 618385-01-6 F: C29H33FN2O4 W: 492.58

Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease
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Bioactivity Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner[1].
Target Ki: 8.1 nM (PAR-1)
Invitro Vorapaxar (SCH 530348) 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 (SCH 530348) 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].
Name Vorapaxar
CAS 618385-01-6
Formula C29H33FN2O4
Molar Mass 492.58
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Reference [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.