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CAS No.: 1194044-20-6

LY2811376 Catalog No. CSN12810

Synonyms: LY2811376

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.

规格	价格	促销价格	库存	数量

400-920-2911

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技术信息

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.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

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 ... more >> 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 Collapse <<

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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.1215 mL
- 15.6074 mL
- 31.2149 mL
- 5 mM
- 0.6243 mL
- 3.1215 mL
- 6.2430 mL
- 10 mM
- 0.3121 mL
- 1.5607 mL
- 3.1215 mL

技术信息

CAS号

1194044-20-6

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H14F2N4S

运输

蓝冰

分子量

320.36

别名

LY2811376

溶解度

DMSO	16.0 mg/mL (49.9 mM)
Water	Insoluble
Ethanol	64.0 mg/mL (199.8 mM)

动物实验配方

30% PEG400+0.5% Tween80+5% propylene glycol+water

30 mg/mL

suspension

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