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].
A-769662 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
3T3-L1
1.2 mM
cytotoxicity assay
decreases Cell Viability
19483304
A-769662 动物研究
Dose
Mice: 30mg/kg[2] (i.p.)
Rats: min = 0.5 mg/kg, max = 10 mg/kg[3] (i.p.)
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