Vorapaxar

Research use only, not for human use.

A potent, selective and orally active thrombin receptor PAR-1 antagonist with Ki of 8.1 nM.

A potent, selective and orally active thrombin receptor PAR-1 antagonist with Ki of 8.1 nM; displays no activity against e PAR-2, PAR-3 and PAR-4, and no CYP450 enzyme inhibition potential; inhibits thrombin (10 nM) induced human platelet aggregation with IC50 of 47 nM; inhibits haTRAP-induced platelet aggregation in vivo.Thrombosis Approved(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 Ki of 1.1 nM. It also inhibits thrombin-stimulated thymidine incorporation in HCASMC with a Ki of 13 nM.

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.

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SCH530348 | SCH-530348 | SCH 530348

GPCR/G Protein

PAR

PAR-1

Cardiovascular Disease

Thrombosis

618385-01-6

492.5817

C29H33FN2O4

>98% (HPLC)

DMSO: ≥ 30 mg/mL

CCOC(=O)NC1CCC2C(C1)CC3C(C2C=CC4=NC=C(C=C4)C5=CC(=CC=C5)F)C(OC3=O)C

Carbamic acid, N-[(1R,3aR,4aR,6R,8aR,9S,9aS)-9-[(1E)-2-[5-(3-fluorophenyl)-2-pyridinyl]ethenyl]dodecahydro-1-methyl-3-oxonaphtho[2,3-c]furan-6-yl]-, ethyl ester

(-20℃)

With Ice Pack

≥ 2 years