AMPK activator
     
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AMPK activator

6,7-Dihydro-4-hydroxy-3-(2'-hydroxy[1,1'-biphenyl]-4-yl)-6-oxo-thieno[2,3-b]pyridine-5-carbonitrile (A-769662)
Potent, reversible AMP-activated protein kinase (AMPK) activator (EC50 = 0.8 ?M) that displays selectivity towards ?1 subunit-containing heterotrimers. Inhibits fatty acid synthesis (IC50 = 3.2 ?M) and decreases plasma glucose and triglyceride levels in vivo.

AMPK_activator
OTAVAchemicals Catalogue Number: 7070707027
CAS Registry Number: 844499-71-4
Purity: 95%+ (HPLC)


Ref.: Cool et al. Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome. Cell Metabolism (2006), 3, 403-416


Abstract: AMP-activated protein kinase (AMPK) is a key sensor and regulator of intracellular and whole-body energy metabolism. We have identified a thienopyridone family of AMPK activators. A-769662 directly stimulated partially purified rat liver AMPK (EC50 = 0.8 microM) and inhibited fatty acid synthesis in primary rat hepatocytes (IC50 = 3.2 microM). Short-term treatment of normal Sprague Dawley rats with A-769662 decreased liver malonyl CoA levels and the respiratory exchange ratio, VCO2/VO2, indicating an increased rate of whole-body fatty acid oxidation. Treatment of ob/ob mice with 30 mg/kg b.i.d. A-769662 decreased hepatic expression of PEPCK, G6Pase, and FAS, lowered plasma glucose by 40%, reduced body weight gain and significantly decreased both plasma and liver triglyceride levels. These results demonstrate that small molecule-mediated activation of AMPK in vivo is feasible and represents a promising approach for the treatment of type 2 diabetes and the metabolic syndrome

 
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