An activator of AMPK heterotrimers (Kd = 9 nM for α1β1γ1); selectively activates β1-containing AMPK isoforms (EC50s = 2.18-7.03 nM) over β2-containing isoforms (EC50s = ≥10 μM); EC50 = 7 nM in an activation/protection TR-FRET assay using α1β1γ1 AMPK; increases phosphorylation of AMPK in rat kidney in vivo at ≥10 mg/kg; decreases urinary albumin levels in a ZSF1 obese rat model of diabetes, metabolic syndrome, and renal disease at 100 mg/kg