Vorapaxar

Vorapaxar is an orally bioavailable competitive antagonist of the proteinase-activated receptor (PAR1, Ki = 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 (Cay-13188) 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.Formal Name: N-[(1R,3aR,4aR,6R,8aR,9S,9aS)-9-[(1E)-2-[5-(3-fluorophenyl)-2-pyridinyl]ethenyl]dodecahydro-1-methyl-3-oxonaphtho[2,3-c]furan-6-yl]-carbamic acid, ethyl ester. CAS Number: 618385-01-6. Molecular Formula: C29H33FN2O4. Formula Weight: 492.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 272, 306 nm. SMILES: C[C@@H](OC1=O)[C@]2([H])[C@@]1([H])C[C@@](C[C@H](NC(OCC)=O)CC3)([H])[C@]3([H])[C@@H]2/C=C/C4=CC=C(C5=CC(F)=CC=C5)C=N4. InChi Code: InChI=1S/C29H33FN2O4/c1-3-35-29(34)32-23-10-11-24-20(14-23)15-26-27(17(2)36-28(26)33)25(24)12-9-22-8-7-19(16-31-22)18-5-4-6-21(30)13-18/h4-9,12-13,16-17,20,23-27H,3,10-11,14-15H2,1-2H3,(H,32,34)/b12-9+/t17-,20+,23-,24-,25+,26-,27+/m1/s1. InChi Key: ZBGXUVOIWDMMJE-QHNZEKIYSA-N.