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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Beta-secretase (BACE)-AZD3839
AZD3839

Chemical Structure : AZD3839

CAS No.: 1227163-84-9

AZD3839 (AZD-3839;AZD 3839)

货号: PC-43534Not For Human Use, Lab Use Only.

AZD3839 (AZD-3839, AZD 3839) is a potent and selective BACE1 inhibitor with Ki of 26 nM, displays 14- and >1000-fold selectivity against BACE2 and cathepsin D.

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10 mg ¥1880 In stock
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50 mg ¥5280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AZD3839 (AZD-3839, AZD 3839) is a potent and selective BACE1 inhibitor with Ki of 26 nM, displays 14- and >1000-fold selectivity against BACE2 and cathepsin D.
AZD3839 inhibits Aβ (Aβ40 IC50=4.8 nM) and sAPPβ release from modified and wild-type human SH-SY5Y cells and mouse N2A cells as well as from mouse and guinea pig primary cortical neurons.
AZD3839 exhibits dose- and time-dependent lowering of plasma, brain, and cerebrospinal fluid Aβ levels in mouse, guinea pig, and non-human primate.
AZD3839 demonstrates significant reduction of β-amyloid peptides in mouse brain.

物理化学性质&存储条件

分子量 431.4125
分子式 C24H16F3N5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1H-Isoindol-3-amine, 1-[2-(difluoromethyl)-4-pyridinyl]-4-fluoro-1-[3-(5-pyrimidinyl)phenyl]-, (1S)-

参考文献

1. Swahn BM, et al. J Med Chem. 2012 Nov 8;55(21):9346-61.

2. Jeppsson F, et al. J Biol Chem. 2012 Nov 30;287(49):41245-57.

3. Aasa J, et al. Drug Metab Dispos. 2013 Jan;41(1):159-69.

4. Sparve E, et al. J Pharmacol Exp Ther. 2014 Aug;350(2):469-78.

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