产品属性:
产品名称 | 规格 | CAS号 | 型号 |
LY2811376 | 5mg 10mg 50mg | 1194044-20-6 | EY-Y0164313 |
Cas No.1194044-20-6
别名
化学名 (4S)-4-(2,4-difluoro-5-pyrimidin-5-ylphenyl)-4-methyl-5,6-dihydro-1,3-thiazin-2-amine
分子式 C15H14F2N4S
![LY2811376.png LY2811376.png](/SupplyImg/2022-11-24/6380488323910273396072046.jpg)
分子量 320.4
溶解度 DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml,Ethanol: 25 mg/ml
储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述:
LY2811376 is a non-peptidic inhibitor of BACE1.
Beta-secretase 1 (BACE1) is an aspartic-acid protease that cleaves the amyloid precursor protein (APP) into amyloid-βpeptide (Aβ), which plays a critical role in Alzheimer's disease (AD).
In recombinant enzyme assays, LY2811376 inhibited hBACE1 with IC50 values of 249 nM and 239 nM against a larger chimeric protein substrate and a small synthetic peptide, respectively. In a human embryonic kidney cell line overexpressed APP, LY2811376 decreased Aβ secretion with EC50 value of 300 nM in a concentration-dependant way [1]. In SH-SY5Y cells, LY2811376 reduced Aβ1-40 and Aβ1-42 secreted to the cell medium while increased the level of Aβ5-40 [2].
In the APPV717F mouse, LY2811376 significantly reduced Aβ, as well as sAPP and C99, the cleavage products of APP by BACE1 [1]. In a healthy population (n =18), LY2811376 (30 mg, 90 mg) increased Aβ5-40 and Aβ5-X in a dose-dependant way, while Aβ1-34 reduced in a same way. These results suggested that LY2811376 inhibited N-terminally truncated Aβ peptides in a BACE1-independent pathway [2].
References:
[1]. May PC, Dean RA, Lowe SL, et al. Robust Central Reduction of Amyloid- in Humans with an
Orally Available, Non-Peptidic -Secretase Inhibitor. J Neurosci, 2011, 31(46): 16507-16516.
[2]. Portelius E, Dean RA, Andreasson U, et al. β-site amyloid precursor protein-cleaving enzyme 1 (BACE1) inhibitor treatment induces Aβ5-X peptides through alternative amyloid precursor protein cleavage. Alzheimers Res Ther, 2014, 6(5-8): 75.
关键字: 1194044-20-6;C15H14F2N4S;LY2811376;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要从事免疫学、分子生物学和常规生化试剂等为一体的科研产品销售企业,公司自成立以来,秉承""全心全意服务于科研工作者""的企业理念,立足生物科技领域,运用生物技术和科研试剂,发展现代生物科技,为各类大中小医院及其它医疗机构、高等院校、科研院所、企事业单位提供优质的产品,服务生物科技领域的科学研究人员。
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