store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Avagacestat (BMS-708163) 是一种有效的γ-secretase 抑制剂,抑制 Aβ42 (IC50:0.27 nM) 和 Aβ40 (IC50:0.30 nM) 的产生。它同时抑制 Notch 胞内结构域 (NICD) (IC50:0.84 nM) 和 CYP2C19 (IC50:20 nM) 。它可用于阿尔兹海默症的研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 479 | 现货 | ||
5 mg | ¥ 935 | 现货 | ||
10 mg | ¥ 1,850 | 现货 | ||
25 mg | ¥ 3,150 | 现货 | ||
50 mg | ¥ 4,620 | 现货 | ||
100 mg | ¥ 6,580 | 现货 | ||
500 mg | ¥ 13,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,110 | 现货 |
产品描述 | Avagacestat (BMS-708163) (BMS-708163) is a potent, selective, orally bioavailable γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, demonstrating a 193-fold selectivity against Notch. Phase 2. |
靶点活性 | γ-secretase (Aβ40):0.3 nM, γ-secretase (Aβ42):0.27 nM |
体外活性 | BMS-708163 exhibits weaker selectivity for inhibition of Notch processing with 193-fold IC50 value. [1] |
体内活性 | Oral administration of BMS-708163 significantly reduces Aβ40 levels for sustained periods in brain, plasma, and cerebrospinal fluid in rats and dogs. BMS-708163 has no dose-limiting effects in dogs (3 mg/kg during 6 months), with a high brain to plasma ratio (2.4). [1] |
细胞实验 | BMS-708163 is dissolved in DMSO. The cell viability is assessed using a tetrazolium salt (WST-8)-based colorimetric assay from the Cell Counting Kit 8 (CCK-8). The cells are seeded into 96-well plates at an initial density of 5×103 cells/well and cultured for 24?h, after which the cells are cultured with DMSO, increased concentrations of gefitinib or BMS708163, BIBW2992, or the combination of BMS708163 and BIBW2992 for an additional 48?h. The A450 is measured in a microplate reader after 10?μL of CCK-8 solution is added and incubated for 1?h. The percentage of growth is shown relative to untreated controls. |
别名 | BMS-708163 |
分子量 | 520.89 |
分子式 | C20H17ClF4N4O4S |
CAS No. | 1146699-66-2 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 96 mg/mL (184.3 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9198 mL | 9.599 mL | 19.1979 mL | 47.9948 mL |
5 mM | 0.384 mL | 1.9198 mL | 3.8396 mL | 9.599 mL | |
10 mM | 0.192 mL | 0.9599 mL | 1.9198 mL | 4.7995 mL | |
20 mM | 0.096 mL | 0.4799 mL | 0.9599 mL | 2.3997 mL | |
50 mM | 0.0384 mL | 0.192 mL | 0.384 mL | 0.9599 mL | |
100 mM | 0.0192 mL | 0.096 mL | 0.192 mL | 0.4799 mL |
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。
Avagacestat 1146699-66-2 Neuroscience Proteases/Proteasome Stem Cells Gamma-secretase BMS-708163 Inhibitor γ-secretase Notch BMS708163 Gamma secretase BMS 708163 inhibit inhibitor