Vorapaxar sulfate

SKU: orb1223074

Description

Vorapaxar sulfate is a potent and orally active thrombin receptor (PAR-1) antagonist.(In Vitro):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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 705260-08-8
• MW: 590.66
• Purity: >98% (HPLC)
• Formula: C₂₉H₃₅FN₂O₈S
• SMILES: S(=O)(=O)(O)O.Fc1cc(c2cnc(/C=C/[C@@H]3[C@H]4[C@@H](C[C@H]5[C@H]3CC[C@@H](NC(=O)OCC)C5)C(=O)O[C@@H]4C)cc2)ccc1
• Target: PAR-1
• Solubility: In Vitro: DMSO : 125 mg/mL (211.63 mM)

Bioactivity

• In Vitro:
  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.
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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

Quick Database Links

Gene Symbol

PAR-1