store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BMS 433796 是一种在阿尔茨海默病转基因小鼠模型中具有Aβ降低活性的γ分泌酶抑制剂,可有效抑制 Aβ 的产生。
产品描述 | BMS 433796 is a γ-secretase inhibitor that demonstrates Aβ-lowering activity within a transgenic mouse model of Alzheimer's disease. |
靶点活性 | Aβ40:0.8 nM, Aβ42:0.4 nM, [3H]-IN973:1.2 nM |
体外活性 | BMS-433796 causes a concentration-dependent decrease in [3H]IN973 binding, with an IC50 value of 1.2 nM, which is very similar to the IC50 values for the inhibition of Aβ40 (0.8 nM) and Aβ42 (0.4 nM) in human embryonic kidney cells overexpressing the Swedish mutation of APP[1]. |
体内活性 | Characterized in pharmacokinetic studies in male Sprague-Dawley rats, BMS-433796 shows low clearance with a total body clearance of 5.2±0.82 mL/min/kg (means±SEM; n=3) following a 10-minute intravenous infusion at 2.3 μmol/kg in PEG-400. The apparent terminal elimination half-life is 4.6±0.48 h. Upon oral administration of a PEG-400 suspension at 35 μmol/kg, BMS-433796 exhibits an oral bioavailability of 31% with prolonged absorption. BMS-433796 demonstrates satisfactory metabolic stability in human liver microsomal preparations and is not an inhibitor of human CYPs (IC50>100 μM)[2]. The reduction of brain Aβ40 is dose-dependent upon administering BMS-433796, with an ED50 value of 2.4 mg/kg[1]. |
别名 | BMS-289948, BMS-299897 |
分子量 | 430.4 |
分子式 | C21H20F2N4O4 |
CAS No. | 935525-13-6 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
BMS 433796 935525-13-6 Neuroscience Beta Amyloid BMS-289948 BMS-299897 BMS-433796 BMS433796 Inhibitor inhibitor inhibit