Allosteric activator of AMP-activated protein kinase (AMPK; EC50 values 0.42 µM and 0.95 µM for increasing the activity of activated heterotrimers α1β1γ1 and α2β1γ1, respectively) that has no effect on mitochondrial function or the ADP/ATP ratio, and which exerts beneficial metabolic effects in vitro and in vivo. ZLN 024 reduced glucose intolerance and fatty liver characteristics in diabetic db/db mice and provides a promising therapeutic approach for type 2 diabetes mellitus and metabolic syndrome.