GCGR Activator

Glybuzole (Desaglybuzole) is an orally effective hypoglycemic agent. Glybuzole promotes insulin secretion by pancreatic β cells and inhibits glucagon secretion by pancreatic α cells. Glybuzole reduces blood glucose levels as well as arginine-stimulated plasma glucagon levels. Glybuzole can be used in diabetes-related research.

GLP-1R modulator-2 is a GLP-1R positive allosteric modulator with an EC₅₀ of 106 nM. GLP-1R modulator-2 simultaneously binds to the extracellular pocket of GLP-1R and the peptide ligand GLP-1 (9-36) through a molecular glue-like allosteric effect, and selectively enhances GLP-1 (9-36)-induced G protein-dependent cAMP signaling. When used in combination with GLP-1 (9-36) under high-glucose conditions, GLP-1R modulator-2 enhances glucose-dependent insulin secretion in wild-type rat pancreatic islets. GLP-1R modulator-2 exhibits strong probe dependence and significantly potentiates the activity of GLP-1 (9-36). GLP-1R modulator-2 can be used for research on type 2 diabetes and obesity .