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BMS 433796

CAS No. : 935525-13-6

MCE 站：BMS 433796

产品活性：BMS 433796 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。

研究领域：Neuronal Signaling  |  Stem Cell/Wnt

作用靶点：γ-secretase

In Vitro: 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.

In Vivo: 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.

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