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Vorapaxar

CAS No. : 618385-01-6

產(chǎn)品活性：Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (K_i=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.

研究領(lǐng)域：GPCR/G Protein

作用靶點(diǎn)：Protease Activated Receptor (PAR)

In Vitro: 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 K_i of 1.1 nM. It also inhibits thrombin-stimulated thymidine incorporation in HCASMC with a Ki of 13 nM.

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