A-769662

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Chemical Structure| 844499-71-4 同义名 : -
CAS号 : 844499-71-4
货号 : A117039
分子式 : C20H12N2O3S
纯度 : 99%+
分子量 : 360.39
MDL号 : MFCD11977269
存储条件：

Pure form Keep in dark place, sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：

IP 2% DMSO+water 3 mg/mL clear

PO 0.5% CMC-Na 35 mg/mL suspension

生物活性
描述 AMPK is a AMP-dependent protein kinase that containsα, β, γ submits, which acts a key role in cellular energy metabolism regulation. A-769662 can activate AMPK reversibly with the EC50 of 0.8 μM in the cell-free assays, and it has little effect on GPPase and FBPase. In vitro, A-769662 was shown to partially stimulate purified rat liver AMPK with an EC50 of 0.8 μM and promote the increased of ACC phosphorylation correlated with inhibition of fatty acid synthesis as measured by incorporation of 14C-acetate into fatty acids, with IC50 3.2μM for A-769662[3]. A-769662 activated AMPK both in cells that express or lack LKB1, without altering adenine nucleotide levels. There are also research reports that A-769662 dose-dependently blocks VGSC in rat TG neurons and in Nav1.7 transfected cells with an IC50 of 10 μM[4]. When treated with SD rats, a single dose of A-769662 can rapidly reduce the expression of hepatic malonyl CoA. In addition, in diabetic ob/ob mice, A-769662 could decrease plasma glucose, triglyceride concentrations and the hepatic expression of the lipogenic enzyme fatty acid synthase as well as the phosphoenolpyruvate carboxykinase (PEPCK) and glucose-6-phosphatase within 5 days[3].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
3T3-L1 1.2 mM Function assay inhibits 3T3-L1 Adipogenesis 19483304
3T3-L1 1.2 mM Function assay inhibits the Expression of AdipogenesisRelated Transcription Factors and Markers 19483304
3T3-L1 1.2 mM Function assay inhibits Mitotic Clonal Expansion 19483304
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.77mL

0.55mL

0.28mL

13.87mL

2.77mL

1.39mL

27.75mL

5.55mL

2.77mL
参考文献

[1]3(6):403-16.

[2]12(1):e0169882.