RO0281675

RO0281675 is a small molecule allosteric activator of **glucokinase (GK)**, an enzyme that serves as a glucose sensor in pancreatic beta cells and hepatocytes. Developed by **Roche**, the compound was designed to treat type 2 diabetes by increasing the affinity of glucokinase for glucose. This mechanism enhances glucose-stimulated insulin secretion from the pancreas and promotes hepatic glucose uptake and glycogen synthesis, thereby lowering blood glucose levels. RO0281675 was used in early clinical development to validate the therapeutic potential of targeting glucokinase, although it was eventually superseded by other candidates in the Roche pipeline, such as piragliatin.

Other names

(2R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N-thiazol-2-yl-propionamide