SML3834

Vorapaxar

≥98% (HPLC)

• 別名: 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
• 実験式（ヒル表記法）: C₂₉H₃₃FN₂O₄
• CAS番号: 618385-01-6
• 分子量: 492.58
• MDL番号: MFCD16038876
• UNSPSCコード: 51111800
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• フォーム: powder
• 色: white to beige
• 溶解性: DMSO: 2 mg/mL, clear
• 保管温度: -10 to -25°C
• SMILES記法: 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 Key: ZBGXUVOIWDMMJE-QHNZEKIYSA-N

詳細

生物化学的／生理学的作用

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.

安全性情報

• ピクトグラム: GHS09
• シグナルワード: Warning
• 危険有害性情報: H410
• 注意書き: P273 - P391 - P501
• 危険有害性の分類: Aquatic Acute 1 - Aquatic Chronic 1
• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable