产品描述: | A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM. |
靶点: |
AMPK:0.8 μM (EC50);AMPK;FattyAcidSynthase |
体内研究: |
A-769662 (30 mg/kg, i.p.) significantly reduced the respiratory exchange ratio (RER) in the SD rat. There are 33% and 58% reductions of malonyl CoA levels in livers of animals treated with 30 mg/kg A-769662 (0.905 nmol/g) or 500 mg/kg metformin (0.574 nmol/g), respectively. A-769662 (30 mg/kg, b.i.d.) significantly decreases fed plasma glucose (30%-40% reduction), while the lower doses (3 and 10 mg/kg) of A-769662 had no effect on the in diabetic ob/ob mice |
参考文献: |
1. Cool B, et al. Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome. Cell Metab, 2006, 3(6), 403-416. 2. Sanders MJ, et al. Defining the mechanism of activation of AMP-activated protein kinase by the small molecule A-769662, a member of the thienopyridone family. J Biol Chem, 2007, 282(45), 32539-32548. 3. Moreno D, et al, A769662, a novel activator of AMP-activated protein kinase, inhibits non-proteolytic components of the 26S proteasome by an AMPK-independent mechanism. FEBS Lett, 2008, 583(17), 2650-2654. [Content Brief] 4. Yerra VG, et al. Adenosine Monophosphate-Activated Protein Kinase Abates Hyperglycaemia-Induced Neuronal Injury in Experimental Models of Diabetic Neuropathy: Effects on Mitochondrial Biogenesis, Autophagy and Neuroinflammation. Mol Neurobiol. 2017 Apr;54 |
溶解性: |
DMSO : 50 mg/mL (138.74 mM; ultrasonic and warming and heat to 80°C) |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.775 ml |
13.874 ml |
27.748 ml |
5 mM |
0.555 ml |
2.775 ml |
5.55 ml |
10 mM |
0.277 ml |
1.387 ml |
2.775 ml |
50 mM |
0.055 ml |
0.277 ml |
0.555 ml |
|
注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |