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LY2886721

CAS No. : 1262036-50-9

MCE 站：LY2886721

产品活性：LY2886721 是一种有效的，选择性的，口服活性的 β 位淀粉样蛋白前体蛋白裂解酶 1 (BACE1) 抑制剂，对重组人 BACE1 的 IC₅₀ 为 20.3 nM。LY2886721 对 BACE1 的选择性高于对组织蛋白酶 D，胃蛋白酶和肾素的选择性，但缺乏对 BACE2 (IC₅₀ 为 10.2 nM) 的选择性。LY2886721 可穿越血脑屏障，并可用于阿尔茨海默氏病的研究。

研究领域：Neuronal Signaling

作用靶点：Beta-secretase

In Vitro: Overnight exposure of HEK293Swe cells to increasing concentrations of LY2886721 shows a concentration-dependent decrease in the amount of Aβ secreted into the condition medium. Consistent with a mechanism of BACE inhibition, the EC₅₀s for inhibition of Aβ_1-40 and Aβ_1-42 are essentially identical, 18.5 and 19.7 nM, respectively.
Overnight exposure of PDAPP neuronal cultures to an increasing concentration of LY2886721 produces a concentration-dependent decrease in Aβ production. As observed in HEK293Swe cells, the EC₅₀s for inhibition of Aβ_1-40 and Aβ_1-42 are comparable in PDAPP neuronal cultures at ?10 nM.

In Vivo: LY2886721 (3-30 mg/kg; oral administration; PDAPP mice) treatment significantly reduces the hippocampal and cortical levels of Aβ_1-x. LY2886721 treatment results in significant reduction of brain parenchymal levels of C99 and sAPPβ.

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