ZLN 024 hydrochloride is an AMPK allosteric activator and stimulates the inactive α1 subunit truncations α1 (1-394) and α1 (1-335) but not α1 (1-312).

AMPK α2β2γ1:0.13 μM (EC50), AMPK α2β1γ1:0.95 μM (EC50), AMPK α1β1γ1:0.42 μM (EC50), AMPK α1β2γ1:1.1 µM (EC50)

ZLN 024 hydrochloride increases the activity of α1β1γ1 by 1.5-fold and has an EC50 of 0.42 µM, and it increases the activity of α2β1γ1 by 1.7-fold with an EC50 of 0.95 µM. ZLN 024 hydrochloride also directly activates recombinant AMPK α1β2γ1, by 1.7-fold with an EC50 of 1.1 µM; and AMPK α2β2γ1, by 1.6-fold with an EC50 of 0.13 µM. ZLN 024 hydrochloride directly activates recombinant AMPK α1β1γ1 and its homolog α2β1γ1 in a concentration-dependent manner[1].

In C57BKS db/db mice, ZLN 024 hydrochloride(15 mg/kg/day; oral) improves glucose tolerance after 4 weeks of treatment. ZLN 024 hydrochloride reduces the fasting blood glucose by 15%. Liver tissue weight, triacylglycerol and the total cholesterol content a