LY2811376
货号:
16712-50mg 基本售价:
12250.0 元 规格:
50 mg
产品信息
概述货号 | 16712-50mg |
描述 | Accumulation of the β-amyloid (Aβ) peptide in the brain is implicated as the primary cause of neurodegeneration and progression of Alzheimer’s disease.1 Aβ is derived from sequential proteolytic cleavage of the amyloid precursor protein (APP) by β-secretase (BACE) and γ-secretase.2 LY2811376 is a non-peptide inhibitor of BACE1 (IC50 = 239 nM for the synthetic peptide) that demonstrates ~10-fold selectivity over BACE2 and >50-fold selectivity over the aspartyl proteases cathepsin D, pepsin, and renin.3 LY2811376 treatment in APP-overexpressing cells and transgenic animal models yields a dose-dependent decrease in Aβ.3 Furthermore, LY2811376 has been reported to reduce C99 and sAPPβ, the two primary APP cleavage products generated by BACE1.3 |
性能供应商 | Cayman |
应用文献 |
1.Hong, L.,Turner, R.T., III,Koelsch, G., et al. Memapsin 2 (β-secretase) as a therapeutic target. Biochemical Society Transactions 30(4), 530-534 (2002). 2.Grüninger-Leitch, F.,Schlatter, D.,Küng, E., et al. Substrate and inhibitor profile of BACE (β-secretase) and comparison with other mammalian aspartic proteases. The Journal of Biological Chemisty 277(7), 4687-4693 (2002). 3.May, P.C.,Dean, R.A.,Lowe, S.L., et al. Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor. Journal of Neuroscience 31(46), 16507-16516 (2011).
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运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 320.4 |
分子式 | C15H14F2N4S |
CAS号 | 1194044-20-6 |
稳定性 | ≥ 2 years |
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