| Vorapaxar Basic information |
| Product Name: | Vorapaxar |
| Synonyms: | Vorapaxar;Vorapaxar (SCH 530348);[(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;Voarapaxar;Ethyl [(1R,3aR,4aR,6R,8aR,9S,9aS)-9-{(E)-2-[5-(3-fluorophenyl)-2-pyridinyl]vinyl}-1-methyl-3-oxododecahydronaphtho[2,3-c]furan-6-yl]carbamate;[(1R,3AR,4aR,6R,8aR,9S,9aS)-9-[(1E)-2-[5-(3-fluorophenyl)-2-pyridinyl]ethenyl]dodecahydro-1-me;Carbamic acid, 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]-, ethyl ester;CS-1663 |
| CAS: | 618385-01-6 |
| MF: | C29H33FN2O4 |
| MW: | 492.58 |
| EINECS: | |
| Product Categories: | API |
| Mol File: | 618385-01-6.mol |
| Vorapaxar Chemical Properties |
| Boiling point | 676.0±55.0 °C(Predicted) |
| density | 1.24±0.1 g/cm3(Predicted) |
| 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) |
| Safety Information |
| MSDS Information |
| Vorapaxar Usage And Synthesis |
| Description | 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 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. |
| Definition | ChEBI: A carbamate ester that is the ethyl ester of [(1R,3aR,4aR,6R,8aR,9S,9aS)-9-{(E)-2-[5-(3-fluorophenyl)pyridin-2-yl]ethyny }-1-methyl-3-oxododecahydronaphtho[2,3-c]furan-6-yl]carbamic acid. A protease-activated receptor-1 antagonist used (as its sulfate salt) for the reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction MI) or with peripheral arterial disease. It has been shown to reduce the rate of a combined endpoint of cardiovascular death, MI, stroke and urgent coronary revascularisation. |
| references | [1]. chackalamannil s & xia, y. thrombin receptor (par-1) antagonists as novel antithrombotic agents. expert opinion on therapeutic patents, 2006.16:493-505.[2]. chackalamannil s, wang y, greenlee w j et al. 2008. discovery of a novel, orally active himbacine-based thrombin receptor antagonist (sch 530348) with potent antiplatelet activity. j med chem, 2008,51: 3061-3064. |
| Vorapaxar Preparation Products And Raw materials |
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