2. Neuronal Signaling Stem Cell/Wnt
  3. γ-secretase
  4. BMS 433796

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。

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BMS 433796 Chemical Structure

BMS 433796 Chemical Structure

CAS No. : 935525-13-6

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BMS 433796 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

BMS 433796 is a γ-secretase inhibitor with Aβ lowering activity in a transgenic mouse model of Alzheimer's disease.

IC50 & Target

γ-secretase[1]
体外研究
(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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

BMS 433796 相关抗体:
体内研究
(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)[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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

430.40

Formula

C21H20F2N4O4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献
Kinase Assay
[2]

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)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

BMS 433796 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMS 433796935525-13-6BMS433796BMS-433796γ-secretaseGamma secretaseInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-50884
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