| Description | Clopidogrel thiolactone (2-oxoclopidogrel) is a potent P2Y12 receptor inhibitor and a potent antiplatelet aggregation compound.Clopidogrel thiolactone is the active metabolic intermediate resulting from the first oxidative activation of Clopidogrel. |
| In vivo | Clopidogrel thiolactone作为一种更强效、更安全的抗血小板药物,可能比氯吡格雷具有以下优势:(1) 对CYP2C19代谢差异者无药物耐药性;(2) 由于有效剂量明显降低,剂量相关毒性更低;(3) 作用起效更快。Clopidogrel thiolactone(8 μm/kg;i.v.;雄性Sprague-Dawley大鼠)表现出良好的生物利用度和药代动力学参数[2]。 |
| Synonyms | 2-oxoclopidogrel |
| molecular weight | 337.82 |
| Molecular formula | C16H16ClNO3S |
| CAS | 1147350-75-1 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: 2 mg/mL (5.92 mM), Sonication and heating are recommended. DMSO: 30 mg/mL (88.80 mM), Sonication is recommended. |
| References | 1. Hagihara K, et al. Comparison of formation of thiolactones and active metabolites of prasugrel and clopidogrel in rats and dogs. Xenobiotica. 2009 Mar;39(3):218-26. 2. Shan J, et, al. Overcoming clopidogrel resistance: discovery of vicagrel as a highly potent and orally bioavailable antiplatelet agent. J Med Chem. 2012 Apr 12;55(7):3342-52. |