LCZ960 is an orally active glucokinase (GK) activator that stimulates GK activity in liver cells in vitro and enhances glucose uptake in vivo by activating hepatic GK. It effectively lowers blood glucose levels in diet-induced obesity (DIO) in mice. LCZ960 maintains normal blood sugar and improves glucose tolerance in DIO mice and rats. Additionally, LCZ960 stimulates glycogen synthase flux and increases glycogen turnover in the liver of rats, inducing an increase in hepatic glycogen cycling. This compound is useful for research on obesity and type 2 diabetes induced by high-fat diets.

LCZ960, administered orally at doses ranging from 0-300 mg/kg either as a single dose or daily for 14-18 days, enhances hepatic glycogen excess plasma levels and glucose tolerance while reducing blood glucose in a diet-induced obesity (DIO) mouse model. A daily oral dose of LCZ960 at 0-30 mg/kg for 7 days lowers blood glucose levels and improves glucose fluctuations in the DIO rat model. Additionally, a single oral dose of 60 mg/kg increases hepatic glycogen storage and synthesis (Vsyn), glycogen breakdown, hepatic glycogen turnover, hepatic glycogen, and plasma glucose, while decreasing plasma lactate concentration in the SD rat model.