A-769662 is a potent, reversible AMP-activated protein kinase (AMPK) activator with an EC50 of 0.8 ¦ÌM.A-769662 displays selectivity towards ¦Â1 subunit-containing heterotrimers. A-769662 not only inhibits fatty acid synthesis with an IC50 of 3.2 ¦ÌM but also decreases plasma glucose and triglyceride levels in vivo. The addition of A-769662 to mouse embryonic fibroblasts or primary mouse hepatocytes stimulates phosphorylation of acetyl-CoA carboxylase (ACC), effects that are completely abolished in AMPK-alpha1(-/-)alpha2(-/-) cells but not in TAK1(-/-) mouse embryonic fibroblasts. Phosphorylation of AMPK and ACC in response to A-769662 is also abolished in isolated mouse skeletal muscle lacking LKB1, a major upstream kinase for AMPK in this tissue. A-769662 directly prevents the alpha(1)-isoform of the Na(+)-K(+)-ATPase which is purified from rat and human kidney cells in vitro with IC50 of 57 ¦ÌM and 220 ¦ÌM, respectively. Suppression of the Na(+)-K(+)-ATPase by 100 ¦ÌM ouabain decreases sodium pump activity and cell surface abundance, similar to the effect of A769662 (A 769662; A-769662), without influencing the phosphorylation of AMPK and ACC

June 21, 2017

prudect name : A-769662 is a potent, reversible AMP-activated protein kinase (AMPK) activator with an EC50 of 0.8 ¦ÌM.A-769662 displays selectivity towards ¦Â1 subunit-containing heterotrimers. A-769662 not only inhibits fatty acid synthesis with an IC50 of 3.2 ¦ÌM but also decreases plasma glucose and triglyceride levels in vivo. The addition of A-769662 to mouse embryonic fibroblasts or primary mouse hepatocytes stimulates phosphorylation of acetyl-CoA carboxylase (ACC), effects that are completely abolished in AMPK-alpha1(-/-)alpha2(-/-) cells but not in TAK1(-/-) mouse embryonic fibroblasts. Phosphorylation of AMPK and ACC in response to A-769662 is also abolished in isolated mouse skeletal muscle lacking LKB1, a major upstream kinase for AMPK in this tissue. A-769662 directly prevents the alpha(1)-isoform of the Na(+)-K(+)-ATPase which is purified from rat and human kidney cells in vitro with IC50 of 57 ¦ÌM and 220 ¦ÌM, respectively. Suppression of the Na(+)-K(+)-ATPase by 100 ¦ÌM ouabain decreases sodium pump activity and cell surface abundance, similar to the effect of A769662 (A 769662; A-769662), without influencing the phosphorylation of AMPK and ACC
A 769662

Synonyms: CAS NO: 844499-71-4Molecular Formula: C₂₀H₁₂N₂O₃SMolecular Weight: 360.39Purity: 98% minSolubility: In DMSOStorage: −20°C

1218778-77-8 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18498464