Vorapaxar , ≥98% , 618385-01-6

CAS NO.：618385-01-6

Empirical Formula: C29H33FN2O4

Molecular Weight: 492.58

MDL number: MFCD16038876

PRODUCT Properties

• Boiling point: 676.0±55.0 °C(Predicted)
• Density: 1.24±0.1 g/cm3(Predicted)
• storage temp.: Store at -20° C
• solubility: ≥24.65 mg/mL in DMSO; insoluble in H2O; ≥10.64 mg/mL in EtOH with ultrasonic
• form: solid
• pka: 12.49±0.60(Predicted)
• color: White to off-white
• InChIKey: ZBGXUVOIWDMMJE-QHNZEKIYSA-N
• SMILES: C(OCC)(=O)N[C@@H]1CC[C@]2([H])[C@@]([H])(C1)C[C@@]1([H])C(=O)O[C@H](C)[C@@]1([H])[C@H]2/C=C/C1=NC=C(C2=CC=CC(F)=C2)C=C1

Description and Uses

Vorapaxar is an orally bioavailable competitive antagonist of the proteinase-activated receptor (PAR1; K_i = 8.1 nM), also known as the thrombin receptor. It is selective for PAR1 over other PARs, as well as a number of GPCRs, ion channels, and receptors. It inhibits platelet aggregation induced by thrombin and haTRAP (IC₅₀s = 47 and 25 nM, respectively). Vorapaxar (0.1 mg/kg, i.v.) completely inhibits platelet aggregation in cynomolgus monkeys ex vivo. Formulations containing vorapaxar are used in the prevention of thrombotic cardiovascular events.

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

Safety

• Symbol(GHS): GHS08,GHS09
• Signal word: Warning
• Hazard statements: H371-H410-H373-H400
• Precautionary statements: P273-P391-P501-P273-P391-P501-P260-P314-P501-P260-P264-P270-P309+P311-P405-P501