mk-3903

Description: MK-3903 is a novel, potent and selective AMPK (AMP-activated protein kinase) activator with EC50 of 8 nM for alpha1 beta1 gamma1 subunit. It activates 10 of the 12 pAMPK complexes with EC50 values in the range of 8-40 nM and maximal activation > 50%. MK-3903 exhibited robust target engagement in mouse liver following oral dosing, leading to improved lipid metabolism and insulin sensitization in mice. Chronic oral administration of MK-3903 robustly increased ACC phosphorylation in liver with more modest effects in skeletal muscle. Treatment of various mouse models with MK-3903 resulted in expected alterations in lipid metabolism and improvements in a measure of insulin sensitization.

References: J Med Chem. 2017 Nov 9; 60(21):9040-9052.