des-fluoro-sitagliptin

Des-fluoro-sitagliptin is a synthetic small molecule and a structural analog of the antidiabetic drug sitagliptin in which a fluorine atom has been removed from the parent compound. It acts as a potent and selective inhibitor of dipeptidyl peptidase-4 (DPP-4), an enzyme that degrades incretin hormones such as glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). By inhibiting DPP-4 activity, des-fluoro-sitagliptin increases circulating levels of active incretins. This leads to enhanced glucose-dependent insulin secretion and reduced glucagon secretion from pancreatic islets. Preclinical studies have shown that des-fluoro-sitagliptin improves glycemic control in animal models of type 2 diabetes mellitus by lowering fasting and postprandial blood glucose levels. Additionally, it has demonstrated beneficial effects on endothelial function and reduction in atherosclerotic lesion formation in mice models. Des-fluoro-sitagliptin also appears to reduce vascular smooth muscle cell proliferation after vascular injury and may have anti-inflammatory properties relevant to macrovascular complications associated with diabetes[2][3][5][8].

Other names

5-desfluoro sitagliptin4-desfluoro sitagliptin(3R)-3-amino-4-(2,4-difluorophenyl)-1-[3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]butan-1-one phosphate