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LY2811376
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LY2811376图片
CAS NO:1194044-20-6
规格:98%
分子量:320.4
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
Non-peptidic BACE1 inhibitor
CAS:1194044-20-6
分子式:C15H14F2N4S
分子量:320.4
纯度:98%
存储:Store at -20°C

Background:

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].
参考文献:
[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.