Vorapaxar

SKU: orb1224439

Description

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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 618385-01-6
• MW: 492.5817
• Purity: >98% (HPLC)
• Formula: C₂₉H₃₃FN₂O₄
• SMILES: CCOC(=O)NC1CCC2C(C1)CC3C(C2C=CC4=NC=C(C=C4)C5=CC(=CC=C5)F)C(OC3=O)C
• Target: PAR
• Solubility: DMSO: ≥ 30 mg/mL

Bioactivity

• 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SCH530348 | SCH-530348 | SCH 530348

Quick Database Links

Gene Symbol

PAR