Sitagliptin-d4 hydrochloride is the deuterium labeled Sitagliptin hydrochloride. This compound is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. It blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition (Kᵢ = 1 nM), thereby increasing active incretin levels. It can also directly stimulate GLP-1 secretion by intestinal L cells, independent of DPP-4, by activating cAMP/PKA and ERK1/2 pathways. Sitagliptin hydrochloride shows protective effects on pancreatic islet grafts in type 1 diabetes models and can be used for studying type 1 and type 2 diabetes.
- This compound can be used as a tracer.
- This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.