A-769662 is a reverible and allosteric activator of AMPK through inhibiting dephosphorylation of AMPK on Thr-172.
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产品名称 | AMPK ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
WZ4003 |
++++
NUAK2, IC50: 100 nM NUAK1, IC50: 20 nM |
98+% | |||||||||||||||||
Dorsomorphin |
++
AMPK, Ki: 109 nM |
99% | |||||||||||||||||
HTH-01-015 |
+++
NUAK1 , IC50: 100 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
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 | |
Dose | Mice: 30mg/kg[2] (i.p.) Rats: min = 0.5 mg/kg, max = 10 mg/kg[3] (i.p.) |
Administration | i.p. |
计算器 | ||||
存储液制备 | ![]() |
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 |
CAS号 | 844499-71-4 |
分子式 | C20H12N2O3S |
分子量 | 360.39 |
SMILES Code | N#CC1=C(O)C(C(C2=CC=C(C3=CC=CC=C3O)C=C2)=CS4)=C4NC1=O |
MDL No. | MFCD11977269 |
别名 | |
运输 | 蓝冰 |
InChI Key | CTESJDQKVOEUOY-UHFFFAOYSA-N |
Pubchem ID | 54708532 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, sealed in dry, room temperature |
溶解方案 |
请根据您的动物给药指南选择适当的溶解方案。 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |
IP 2% DMSO+water 3 mg/mL clear PO 0.5% CMC-Na 35 mg/mL suspension |