Ro 28-0450

Ro 28-0450 is a small molecule, racemic glucokinase activator (GKA) originally developed by Hoffmann-La Roche. It acts as an allosteric activator of glucokinase (GK, hexokinase IV), which serves as a glucose sensor in pancreatic beta cells and hepatocytes. By binding to an allosteric site on glucokinase, Ro 28-0450 increases the enzyme's affinity for glucose and its maximum velocity ($V_{max}$), thereby enhancing glucose-stimulated insulin secretion and hepatic glucose utilization. The compound is a racemic mixture, with its R-enantiomer, Ro 28-1675, being the active form, while the S-enantiomer is inactive. It is primarily used as a research tool to study glucose homeostasis, insulin secretion, and metabolic pathways in models of type 2 diabetes.

Other names

(±)-RO 28-16753-Cyclopentyl-2-(4-methanesulfonyl-phenyl)-N-thiazol-2-yl-propionamide