LY2121260

LY2121260 is a novel, enantiopure small-molecule glucokinase activator (GKA) developed by Eli Lilly (Lilly Research Laboratories). It acts as a positive allosteric modulator of glucokinase (GK), binding to an allosteric site in the hinge region of the enzyme. By increasing the affinity of glucokinase for glucose and enhancing its maximal velocity (Vmax), LY2121260 stimulates glucose-dependent insulin secretion in pancreatic beta-cells and increases glucose utilization and glycogen synthesis in hepatocytes. Preclinical studies in rat models demonstrated that oral administration of LY2121260 significantly improves glucose tolerance and reduces blood glucose levels after an oral glucose challenge. It has been primarily investigated for the treatment of type 2 diabetes, though its clinical development was not pursued.

Other names

2-(S)-cyclohexyl-1-(R)-(4-methanesulfonyl-phenyl)-cyclopropanecarboxylic acid thiazol-2-ylamide2-cyclohexyl-1-(4-methanesulfonylphenyl)cyclopropanecarboxylic acid thiazol-2-ylamide