ELN318463,851600-86-7

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ELN318463

CAS No. : 851600-86-7

MCE 国际站：ELN318463

产品活性：ELN318463 是淀粉样前体蛋白 (APP) 选择性的 γ-分泌酶 (γ-secretase) 抑制剂。ELN318463 对包含早老蛋白 (PS1) 和 PS2 的 γ-分泌酶抑制活性不同，对 PS1 和 PS2 的 EC₅₀ 分别为 12 nM 和 656 nM。ELN318463 对 PS1 的选择性比对 PS2 高约 51 倍。

研究领域：Neuronal Signaling  |  Stem Cell/Wnt

作用靶点：γ-secretase

In Vitro: ELN318463 behaves as a classic γ-secretase inhibitor, demonstrates 75- to 120-fold selectivity for inhibiting Aβ production compared with Notch signaling in cells, and displaces an active site directed inhibitor at very high concentrations only in the presence of substrate.

In Vivo: ELN318463 (30 mg/kg or 100 mg/kg; orally) leads acute reduction of brain Aβ in in the PDAPP transgene model of Alzheimer's disease (AD) as well as in wild-type FVB strain mice.

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