| Bioactivity | 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]. |
| Target | Ki: 8.1 nM (PAR-1) |
| Invitro | 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]. |
| Name | Vorapaxar sulfate |
| CAS | 705260-08-8 |
| Formula | C29H35FN2O8S |
| Molar Mass | 590.66 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 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. |