產(chǎn)品目錄

規(guī)格	5mg 10mg 50mg
CAS	1227163-84-9
別名
化學(xué)名	(S)-3-(2-(difluoromethyl)pyridin-4-yl)-7-fluoro-3-(3-(pyrimidin-5-yl)phenyl)isoindolin-1-imine
分子式	C24H16F3N5
分子量	431.41
溶解度	DMF: 2 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS (pH 7.2) (1:1): 0.5 mg/ml
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

Description:

IC50: 16.7 nM for BACE1

β-Site amyloid precursor protein cleaving enzyme1 (BACE1) is one of the key enzymes involved in the processes of the amyloid precursor protein (APP) and formation of amyloid β peptide (Aβ) species. Because cerebral deposition of Aβ species is possibly critical for the pathogenesis of Alzheimer disease, BACE1 has emerged as a key target for the treatment of this disease. AZD3839 is a potent and selective BACE1 inhibitor.

In vitro: AZD3839 concentration-dependently inhibited BACE1 activity in a biochemical fluorescence resonance energy transfer assay, Aβ and sAPPβ release from modified and wild-type human SH-SY5Y cells and mouse N2A cells as well as from guinea pig and mouse primary cortical neurons. Selectivity against BACE2 and cathepsin D was 14 and >1000-fold, respectively [1].

In vivo: AZD3839 exhibited dose- and time-dependent lowering of plasma, brain, and cerebrospinal fluid Aβ levels in mouse, guinea pig, and non-human primate. PK/PD analyses of mouse and guinea pig data showed a good correlation between the potency of AZD3839 in primary cortical neurons and in vivo brain effects [1].

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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