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LY2811376 {[allProObj[0].p_purity_real_show]}

货号:A423338

LY2811376 is the first orally available non-peptidic β-secretase (BACE1) inhibitor with IC50 of 239 nM-249 nM, that acts to decrease Aβ secretion with EC50 of 300 nM, and demonstrates to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin.

LY2811376 化学结构 CAS号:1194044-20-6
LY2811376 化学结构
CAS号:1194044-20-6
LY2811376 3D分子结构
CAS号:1194044-20-6
LY2811376 化学结构 CAS号:1194044-20-6
LY2811376 3D分子结构 CAS号:1194044-20-6
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LY2811376 纯度/质量文件 产品仅供科研

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LY2811376 生物活性

描述 LY2811376 is the first orally available non-peptidic β-secretase (BACE1) inhibitor with IC50 of 239 nM-249 nM, that acts to decrease Aβ secretion with EC50 of 300 nM, and demonstrates to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin.

LY2811376 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
HEK293 cells Function assay Inhibition of BACE1 in HEK293 cells expressing APPswedish mutant assessed as inhibition of amyloid beta production by ELISA, EC50=0.3 μM 24704031

LY2811376 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00838084 Alzheimer's Disease Phase 1 Completed - United States, California ... 展开 >> For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Glendale, California, United States 收起 <<

LY2811376 参考文献

[1]Zhang X, Tian Y, et al. Near-infrared fluorescence molecular imaging of amyloid beta species and monitoring therapy in animal models of Alzheimer's disease. Proc Natl Acad Sci U S A. 2015 Aug 4;112(31):9734-9.

[2]May PC, Dean RA, et al. Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor. J Neurosci. 2011 Nov 16;31(46):16507-16.

LY2811376 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.12mL

0.62mL

0.31mL

15.61mL

3.12mL

1.56mL

31.21mL

6.24mL

3.12mL

LY2811376 技术信息

CAS号1194044-20-6
分子式C15H14F2N4S
分子量 320.36
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,2-8°C

溶解度

DMSO: 30 mg/mL(93.64 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方

30% PEG400+0.5% Tween80+5% propylene glycol+water 30 mg/mL suspension

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