化合物Avagacestat T6249

Product Introduction
Bioactivity


英文名: Avagacestat

描述: 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。

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.

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]

存储条件: store at low temperaturePowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 96 mg/mL (184.3 mM)


关键字: Inhibitor | γ-secretase | Avagacestat | Notch | BMS708163 | Gamma secretase | BMS 708163 | inhibit

相关产品: FLI-06 | Aβ42-IN-2 | Rovalpituzumab | Demcizumab | Carvacrol | Fosciclopirox | YO-01027 | LY-411575 | ELN318463 racemate | Ro 90-7501

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Human Metabolite Library | Neuronal Signaling Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Protease Inhibitor Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途