A-769662 (CAS 844499-71-4), >99%

LC Laboratories' Product Number A-1803 - A-769662 (CAS 844499-71-4), >99% - for research use only. A-769662 is a potent, reversible activator of AMP-activated protein kinase (AMPK). AMPK is an αβγ heterotrimer and plays an important role in regulating cellular and whole-body metabolism. A-769662 only activates AMPK heterotrimers containing the β1 subunit. A-769662 activates AMPK through the β subunit carbohydrate-binding module and the γ subunit but not the AMP-binding sites. A-769662 stimulated partially purified rat liver AMPK with an EC50 of 0.8 µM and inhibited fatty acid synthesis in primary rat hepatocytes with an IC50 of 3.2 µM. A-769662 decreased liver malonyl CoA levels of Sprague Dawley rats and the respiratory exchange ratio, VCO2/VO2, and thus increased rate of whole-body fatty acid oxidation. A-769662 reduced hepatic expression of PEPCK, G6Pase, and FAS, decreased body weight gain, lowered plasma glucose by 40%, and reduced both plasma and liver triglyceride levels in ob/ob mice. A-769662 induces allosteric activation of AMP-activated protein kinase (AMPK) and inhibition of dephosphorylation of AMPK on Thr-172, similar to the effects of AMP. The effects of A-769662 are not dependent on the upstream kinase used in intact cells. In skeletal muscle, A-769662 activates β1-containing AMPK complexes, but induces glucose uptake via a PI3 kinase-dependent pathway. A-769662 inhibits 3T3-L1 adipocyte differentiation and may be used to treat obesity. A-769662 inhibited the function of the 26S proteasome via an AMPK-independent mechanism.

• Supplier: LC Laboratories
• Product #: A-1803
• Sku #: A-1803_25mg