| 中文名称: | BMS 433796 | ||||
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| 英文名称: | BMS 433796 | ||||
| 别名: | (S)-2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetamido)-N-((S)-3-methyl-4-oxo-4,5-dihydro-3H-benzo[d][1,2]diazepin-5-yl)propanamide | ||||
| CAS No: | 935525-13-6 | 分子式: | C19H16F2N4O4 | 分子量: | 402.35 |
| CAS No: | 935525-13-6 | ||||
| 分子式: | C19H16F2N4O4 | ||||
| 分子量: | 402.35 | ||||
基本信息
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产品编号： |
B11703 |
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产品名称： |
BMS 433796 |
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CAS: |
935525-13-6 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
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分子量 |
402.35 |
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化学名： |
(S)-2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetamido)-N-((S)-3-methyl-4-oxo-4,5-dihydro-3H-benzo[d][1,2]diazepin-5-yl)propanamide |
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Solubility (25°C)： |
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体外:
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DMSO |
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Water |
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Ethanol |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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生物活性
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产品描述 |
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。 |
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靶点 |
γ-secretase |
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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 |
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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)[1]. 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 |
推荐实验方法(仅供参考)
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Kinase Assay |
The binding assay is performed in duplicate in an assay volume of 250 μl consisting of 25 μL of buffer (50 mM HEPES and 0.1% CHAPSO, pH 7.0) or 10 μM BMS-433796 to define nonspecific binding, 25 μL of buffer containing [3H]IN973, and 200 μL of homogenate (200 μg of protein). Incubation is initiated by the addition of the membrane homogenates at 25°C for 1 h. Binding reactions are terminated by filtration through Whatman GF/B filters using a cell harvester. Unbound radioactivity is removed by rinsing the filters with ice-cold wash buffer (PBS; pH 7.0). Filters are counted using a 2500TR liquid scintillation counter. Saturation data are analyzed by the nonlinear regression analysis program LIGAND. Binding curves are best fit to a one-site model, yielding the equilibrium dissociation constant (Kd) and the maximal number of binding sites (Bmax) |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
