中文名称: BMS 433796
英文名称: BMS 433796
CAS No: 935525-13-6
分子式: C19H16F2N4O4
分子量: 402.35
B11703 BMS 433796 (psaitong)
包装规格:
100mg in glass bottle
产品简介:
是一种 γ-分泌酶抑制剂,用于阿尔茨海默氏病转基因小鼠模型,可降低 Aβ 活性。
靶点:
γ-secretase
体外研究:
BMS-433796 cause a concentration-dependent decrease in [3H]IN973 binding, with IC50 value of 1.2 nM, very similar to the IC50 values for inhibition of Aβ40 in human embryonic kidney cells overexpressing the Swedish mutation of APP of 0.8 nM, respectively, and for inhibition of Aβ42 of 0.4 nM, respectively.
体内研究:
BMS 433796 is characterized in pharmacokinetic studies in male Sprague-Dawley rats. Following a 10-min intravenous infusion at 2.3 μmol/kg in PEG-400, the total body clearance of 40 is 5.2±0.82 mL/min/kg (means±SEM; n=3), indicating low clearance. The apparent terminal elimination half-life is 4.6±0.48 h. Oral administration of a PEG-400 suspension at 35 μmol/kg shows an oral bioavailability of 31% with prolonged absorption. BMS 433796 has satisfactory metabolic stability in human liver microsomal preparations and is not an inhibitor of human CYPs (IC50>100 μM). Brain Aβ40 is reduced as a result of administering BMS-433796 in a dose-dependent manner, with ED50 value of 2.4 mg/kg, respectively.
保存条件:
-20℃
注意事项:
1、为了您的安全和健康,请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
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