AZD3839

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AZD3839

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1227163-84-9

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
50mg	电议

产品介绍

AZD3839 是一种有效的、选择性的口服活性、脑渗透性 BACE1 抑制剂 (Ki=26 nM)。 AZD3839 对 BACE2 和组织蛋白酶 D 的选择性分别为 14 倍和 >1000 倍。 AZD3839 表现出血浆、脑和脑脊液的剂量和时间依赖性降低 Aβ；小鼠、豚鼠和非人类灵长类动物中的水平。 AZD3839可用于Alzheimer's病的研究。

Cas No.	1227163-84-9
化学名	(S)-3-(2-(difluoromethyl)pyridin-4-yl)-7-fluoro-3-(3-(pyrimidin-5-yl)phenyl)isoindolin-1-imine
Canonical SMILES	FC1=CC=CC([C@@]2(C3=CC(C(F)F)=NC=C3)C4=CC=CC(C5=CN=CN=C5)=C4)=C1C(N2)=N
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
储存条件	Store at -20℃
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
产品描述	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]. Clinical trial: Based on the pharmacological profile and its drug like properties, AZD3839 has been progressed into Phase 1 clinical trials in man [2]. Reference: [1] Jeppsson F, Eketj?ll S, Janson J, Karlstr?m S, Gustavsson S, Olsson LL, Rades?ter AC, Ploeger B, Cebers G, Kolmodin K, Swahn BM, von Berg S, Bueters T, F?lting J. Discovery of AZD3839, a potent and selective BACE1 inhibitor clinical candidate for the treatment of Alzheimer disease. J Biol Chem. 2012 Nov 30;287(49):41245-57. [2] https://clinicaltrials. gov/ct2/show/NCT01348737?term=AZD3839&rank=1