Sitagliptin

Description

Sitagliptin MK-0431 is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 GLP-1 and glucose-dependent insulinotropic peptide GIP by competing inhibition mechanism K? = 1 nM , thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.