产品说明书

AZD3839

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Chemical Structure| 1227163-84-9 同义名 : AZD3839 free base
CAS号 : 1227163-84-9
货号 : A886914
分子式 : C24H16F3N5
纯度 : 99%+
分子量 : 431.413
MDL号 : MFCD25976574
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(278.16 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 AZD3839 free base is a potent and selective orally active BACE1 inhibitor that penetrates the brain (Ki=26 nM). It demonstrates a 14-fold selectivity against BACE2 and >1000-fold selectivity against cathepsin D. AZD3839 free base effectively reduces plasma, brain, and cerebrospinal fluid Aβ levels in mouse, guinea pig, and non-human primate models in a dose- and time-dependent manner. It holds promise for Alzheimer's disease research[1][2].
作用机制 AZD3839 binds in the active site of BACE1 in a flap-open conformation with the pyridine nitrogen located close to the S2 pocket, interacting with Trp-76 via an important hydrogen bond.[1]
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
CHO cells Function assay Inhibition of human ERG expressed in CHO cells by IonWorks assay, IC50=4.8 μM 22924815
SH-SY5Y cells Function assay 16 h Inhibition of BACE1 in human SH-SY5Y cells assessed as inhibition of sAPPbeta release after 16 hrs by immunoassay, IC50=0.0167 μM 22924815
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.32mL

0.46mL

0.23mL

11.59mL

2.32mL

1.16mL

23.18mL

4.64mL

2.32mL
参考文献

[1]Sparve E et al. Prediction and modeling of effects on the QTc interval for clinical safety margin assessment, based on single-ascending-dose study data with AZD3839. J Pharmacol Exp Ther. 2014 Aug;350(2):469-78.

[2]Jeppsson F et al. 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.