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Vorapaxar and M20 completely blocked thrombin-stimulated PAR1/β-arrestin association in recombinant cells and abolished thrombin-stimulated calcium influx in washed human platelets and vascular smooth muscle cells. Moreover, vorapaxar and M20 inhibited PAR1 agonist peptide-mediated platelet aggregation in human platelet rich plasma with a steep concentration response relationship. Vorapaxar exhibited high selectivity for inhibition of PAR1 over other platelet GPCRs.
| Molecular Weight | 590.66 |
| Formula | C29H35FN2O8S |
| CAS Number | 705260-08-8 |
| Solubility (25°C) | DMSO 75 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PAR Products |
|---|
| ML161
Parmodulin 2 (ML161) is an allosteric inhibitor of PAR1 with IC50 of 0.26 μM. |
| Vorapaxar
Vorapaxar (SCH 530348) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nM. |
| ML354
ML354 is a potent and selective PAR4 (protease activated receptor-4) antagonist. |
| PAR-4 (1-6) (human)
PAR-4 (1-6) (human) is an N-terminal fragment of protease-activated receptor 4 (PAR4) that acts as a PAR4 agonist. |
| PAR-4 (1-6) (mouse)
PAR-4 (1-6) (mouse) |
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