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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 |
|---|
| SCH79797 dihydrochloride
SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. |
| TRAP-6 amide
TRAP-6 amide is a PAR-1 thrombin receptor agonist peptide. |
| Protease-Activated Receptor-1, PAR-1 Agonist
Protease-Activated Receptor-1, PAR-1 Agonist is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. |
| FSLLRY-NH2
FSLLRY-NH2 is a protease-activated receptor 2 (PAR2) inhibitor. |
| iso-TRAP-6
iso-TRAP-6 (iso-SFLLRN) is a PAR-1 agonist that can activate platelets. |
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