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E2012
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产品介绍
产品介绍
产品信息
简单描述
A γ-secretase modulator
商品描述
E2012 is a modulator of γ-secretase.1 It selectively inhibits APP intracellular signaling domain (AICD) cleavage to amyloid-β (Aβ) over Notch cleavage to its signaling effector Notch intracellular domain (NICD), processes both mediated by γ-secretase, when used at a concentration of 1 µM in luciferase assays.2 E2012 also inhibits the activity of the cholesterol synthesis enzyme 3β-hydroxysterol ∆24-reductase (DHCR24) in primary rat hepatocytes and HepG2 cells (IC50s = 11 and 15 nM, respectively).3 It reduces Aβ (1-42) (Aβ42) production in primary rat embryonic cerebral cortex neurons with an IC50 value of 220 nM.4 E2012 (100 mg/kg) also decreases Aβ42 levels in guinea pig brain and cerebral spinal fluid (CSF).4
分子量
419.5
纯度
≥98%
背景
结构式
FC1=CC=C([C@H](C)N2C(/C(CCC2)=C/C3=CC(OC)=C(N4C=NC(C)=C4)C=C3)=O)C=C1
分子式
C25H26FN3O2
CAS号
870843-42-8
制备和贮存
保存
≥ 4 years
溶解方法
DMF: 10mg/mL
DMSO: 10mg/mL
DMSO:PBS (pH 7.2) (1:3): 0.25mg/mL
Ethanol: 10mg/mL
保存方式
-20°C
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