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A-769662 {[allProObj[0].p_purity_real_show]}

货号:A117039

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

A-769662 化学结构 CAS号:844499-71-4
A-769662 化学结构
CAS号:844499-71-4
A-769662 3D分子结构
CAS号:844499-71-4
A-769662 化学结构 CAS号:844499-71-4
A-769662 3D分子结构 CAS号:844499-71-4
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A-769662 纯度/质量文件 产品仅供科研

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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。

A-769662 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].

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.)
Administration i.p.

A-769662 参考文献

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

[2]12(1):e0169882.

A-769662 实验方案

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

A-769662 技术信息

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
方案一
方案二
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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