PSN-GK1

PSN-GK1 is a potent, small molecule glucokinase activator (GKA) originally developed by Prosidion (a subsidiary of OSI Pharmaceuticals) for the treatment of type 2 diabetes. It acts as a positive allosteric modulator of glucokinase (hexokinase IV), an enzyme that serves as a glucose sensor in pancreatic beta cells and the liver. By increasing the affinity of glucokinase for glucose, PSN-GK1 enhances glucose-stimulated insulin secretion and promotes hepatic glucose uptake and glycogen synthesis. In preclinical studies using diabetic rodent models such as db/db mice and Zucker diabetic fatty rats, the compound demonstrated significant antihyperglycemic effects with high oral bioavailability and without inducing hypoglycemia. Despite its potency and favorable pharmacokinetic profile in research settings, PSN-GK1 did not progress into clinical development and is primarily utilized as a pharmacological tool in metabolic research.

Other names

(2R)-2-(4-cyclopropanesulfonylphenyl)-N-(5-fluorothiazol-2-yl)-3-(tetrahydropyran-4-yl)propionamideCAS 745051-61-0CAS745051-61-0CAS-745051-61-0