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CAS No.: 844499-71-4

A-769662 Catalog No. CSN12424

Synonyms: A-769662

A-769662 is a reverible and allosteric activator of AMPK through inhibiting dephosphorylation of AMPK on Thr-172.

规格	价格	促销价格	库存	数量

400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 AMPK

EC50:0.8μM
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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

更多
动物研究
剂量
Mice: 30mg/kg^[2] (i.p.) Rats: min = 0.5 mg/kg, max = 10 mg/kg^[3] (i.p.)

给药途径
i.p.

动物研究
剂量	Mice: 30mg/kg^[2] (i.p.) Rats: min = 0.5 mg/kg, max = 10 mg/kg^[3] (i.p.)
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7748 mL
- 13.8740 mL
- 27.7480 mL
- 5 mM
- 0.5550 mL
- 2.7748 mL
- 5.5496 mL
- 10 mM
- 0.2775 mL
- 1.3874 mL
- 2.7748 mL

技术信息

CAS号

844499-71-4

储存条件

粉末: Keep in dark place,Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H12N2O3S

运输

蓝冰

分子量

360.39

别名

A-769662

溶解度

DMSO	180.0 mg/mL (499.5 mM) warming
Water	2.0 mg/mL (5.5 mM) warming

动物实验配方

IP	2% DMSO+water	3 mg/mL	clear
PO	0.5% CMC-Na	35 mg/mL	suspension

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

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
3T3-L1	1.2 mM	Kinase assay	-	activates AMPK	19483304
BT474	400 μM	Apoptosis assay	-	sensitizes human breast cancer cell lines to TRAIL-induced apoptosis	19896469
CCL13	200 μM	Kinase assay	-	activates endogenous AMPK	17728241
epididymal clear cells	200 μM	Function assay	-	inhibits the pH-mediated V-ATPase accumulation at the apical membrane	19211918
HEK293	200 μM	Kinase assay	-	activates endogenous AMPK	17728241
L6 skeletal muscle cells	250 μM	Function assay	-	activates AMPK signaling pathways	19828836
L6 skeletal muscle cells	250 μM	Function assay	-	inhibits the Na+-K+-ATPase transport activity and cell surface abundance	19828836
MC3T3-E1	10 µM	cytotoxicity assay	-	inhibits H2O2-Induced Osteoblast Cell Death	24960362
MC3T3-E1	10 µM	Apoptosis assay	-	suppresses H2O2-Induced Osteoblast Cell Apoptosis	24960362
MC3T3-E1	10 µM	Function assay	-	alleviates ROS accumulation and ATP depletion caused by H2O2	24960362
MC3T3-E1	10 µM	Function assay	-	facilitates H2O2-induced autophagy activation	24960362
MC3T3-E1	10 μM	Kinase assay	-	induces significant AMPK activation	26891866
MC3T3-E1	10 μM	Growth inhibitory assay	-	inhibits Dex-induced osteoblast cell death	26891866
MC3T3-E1	10 μM	Function assay	-	inhibits Dex-induced oxidative stress	26891866
MCF7	400 μM	Apoptosis assay	-	sensitizes human breast cancer cell lines to TRAIL-induced apoptosis	19896469
MDA-MB231	400 μM	Apoptosis assay	-	sensitizes human breast cancer cell lines to TRAIL-induced apoptosis	19896469
MEFs	300 μM	Function assay	-	inhibits proteasomal function by an AMPK-independent mechanism	18593584
Mesenchymal stem cells	10 µM	Kinase assay	-	induces a robust and sustained AMPK activation	24104879
Mesenchymal stem cells	100 µM	cytotoxicity assay	-	decreases the MSC proliferation	24104879
MG-63	10 µM	cytotoxicity assay	-	inhibits H2O2-Induced Osteoblast Cell Death	24960362
MG-63	10 µM	Apoptosis assay	-	suppresses H2O2-Induced Osteoblast Cell Apoptosis	24960362
MG-63	10 µM	Function assay	-	alleviates ROS accumulation and ATP depletion caused by H2O2	24960362
MG-63	10 µM	Function assay	-	facilitates H2O2-induced autophagy activation	24960362
mouse hepatocytes	1 mM	Function assay	-	inhibits fatty acid synthesis with IC50 of 3.6 μM	16753576
PC3	100 µM	Kinase assay	-	upregulates the levels of AMPK and ACC phosphorylation	25594043
PC3	100 µM	Function assay	-	induces PI3K/mTOR pathways	25594043
PC3	100 µM	Growth inhibitory assay	-	suppresses proliferation	25594043
PC3M	100 µM	Kinase assay	-	upregulates the levels of AMPK and ACC phosphorylation	25594043
PC3M	100 µM	Function assay	-	induces PI3K/mTOR pathways	25594043
PC3M	100 µM	Growth inhibitory assay	-	suppresses proliferation	25594043
rat hepatocytes	1 mM	Function assay	-	inhibits fatty acid synthesis with IC50 of 3.6 μM	16753576

A-769662 Catalog No. CSN12424

靶点选择性

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