SML3834

Vorapaxar

≥98% (HPLC)

• Sinonimo/i: Ethyl [(3aR,4aR,8aR,9aS)-9(S)-[(E)-2-[5-(3-fluorophenyl)-2-pyridinyl]ethenyl]dodecahydro-1(R)-methyl-3-oxonaphtho[2,3-c]furan-6(R)-yl]carbamate, MK 5348, MK-5348, MK5348, SCH 530348, SCH-530348, SCH530348
• Formula empirica (notazione di Hill): C₂₉H₃₃FN₂O₄
• Numero CAS: 618385-01-6
• Peso molecolare: 492.58
• Numero MDL: MFCD16038876
• Codice UNSPSC: 51111800
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥98% (HPLC)
• Stato: powder
• Colore: white to beige
• Solubilità: DMSO: 2 mg/mL, clear
• Temperatura di conservazione: -10 to -25°C
• Stringa SMILE: Fc1cc(ccc1)c2cnc(cc2)\C=C\[C@@H]3[C@H]4[C@@H](C[C@H]5[C@H]3CC[C@H](C5)NC(=O)OCC)C(=O)O[C@@H]4C
• InChI: ZBGXUVOIWDMMJE-QHNZEKIYSA-N

Descrizione

Azioni biochim/fisiol

Orally active, potent and selective thrombin receptor (PAR-1) antagonist with anti-platelet aggregation efficacy in vitro and in vivo.

Vorapaxar (MK-5348; SCH 530348) is an orally active, potent and selective thrombin receptor (PAR-1) antagonist with good selectivity over a panel of GPCRs, ion channels, and receptors, including PAR-2, PAR-3 and PAR-4. Vorapaxar inhibitis thrombin-induced calcium transient and thymidine incorporation in human coronary artery smoothmuscle cells (HCASMC; Ki = 1.1 and 13 nM, respectively), as well as aggregation in human platelet-rich plasma (PRP) induced by 10 nM thrombin or 15 μM haTRAP (IC50 = 47 and 25 nM, respectively), but not 20 μM ADP or 5 μM collagen. Oral administration (0.1 mg/kg to cynomolgus monkeys) prevents haTRAP-induced platelet aggregation ex vivo.

Informazioni sulla sicurezza

• Pittogrammi: GHS09
• Avvertenze: Warning
• Indicazioni di pericolo: H410
• Consigli di prudenza: P273 - P391 - P501
• Classi di pericolo: Aquatic Acute 1 - Aquatic Chronic 1
• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable