AMPK activator 4 is a potent and selective AMPK activator that does not inhibit mitochondrial complex I. It selectively activates AMPK in muscle tissue, dose-dependently improves glucose tolerance in normal mice, significantly reduces fasting glucose levels, and improves insulin resistance in db/db diabetic mice. [AMPK activator 4 has hypoglycemic effects.]

AMPK activator 4 (compound B10) (10-20 μM; 72 h) slightly decreases the viability of HepG2 cells. [1] AMPK activator 4 (0-20 μM; 12-24 h) induces dose-dependent phosphorylation of ACC in C2C12 myotube cells, with this phosphorylation being consistent with AMPK phosphorylation. Additionally, it increases AMPK and ACC phosphorylation in HepG2 and HuH-7 cells. [1]

AMPK activator 4 (100 mg/kg; intragastrical administration; daily for 9 weeks; db/db mice) significantly lowered fasting blood glucose in db/db mice (2-6 weeks) and significantly improved insulin resistance (for 9 weeks), without significantly affecting body weight or serum levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST), demonstrating an anti-hyperglycemic effect.[1]