化合物LY2886721 T6058

Product Introduction
Bioactivity


英文名: LY2886721

描述: LY2886721 是选择性的，口服活性的 β 位淀粉样蛋白前体蛋白裂解酶 1 抑制剂，对重组人 BACE1的 IC50=20.3 nM。它对 BACE1的选择性高于对组织蛋白酶 D、胃蛋白酶、肾素的选择性，但缺乏对 BACE2的选择性。它可透过血脑屏障，并可用于研究阿尔茨海默氏病。

激酶实验: The CTLs and NK cells (0.8×106/mL) are treated with the inhibitors L1 (10-20 μM) or Aloxistatin (20-30 μM) for 24 hr at 37°C in 24-well plates. Cells are then used in 51Cr-release assays or are lysed to examine perforin in Western blots. The inhibitor is also added at the same concentration during the 4 hr reactions in some 51Cr-release assays, as indicated. Cell lysates are prepared using NP-40 lysis buffer (25 mM HEPES, 250 mM NaCl, 2.5 mM ethylenediaminetetraacetic acid, 0.1% volume/volume Nonidet P-40) and total protein concentration is determined using the Bradford assay. Equal amounts of protein are loaded and resolved on 8% SDS-PAGE gels. Human or mouse perforin is detected using the appropriate antibodies as indicated. Anti-actin antibody is used as a loading control[2].

体外活性: LY2886721 is an oral, small molecule of β-site amyloid protein cleaving enzyme (BACE) inhibitor with the potential to inhibit the synthesis of β-amyloid and thereby to slow the Clinicalal progression of AD. [1] LY2886721 can also targetγ-secretase to nhibit the synthesis of β-amyloid. [2]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 9 mg/mL (23.05 mM)


关键字: BACE2 | Inhibitor | BACE | Beta-secretase | BBB | Alzheimer's | BACE1 | sAPPβ | LY 2886721 | LY2886721 | C99 | LY-2886721 | inhibit | disease | β-Secretase

相关产品: Cassiaside | Sophoflavescenol | Eslicarbazepine Acetate | LY2811376 | Eslicarbazepine | Se-Methylselenocysteine hydrochloride | LX2343 | Epiberberine chloride | Aloeresin D | Aloenin

相关库: Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | Clinical Compound Library | CNS-Penetrant Compound Library | Neuronal Signaling Compound Library | Inhibitor Library | Anti-Cardiovascular Disease Compound Library | Covalent Inhibitor Library | Bioactive 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