DPP-IV-IN-1 is a potent inhibitor of dipeptidyl peptidase IV (DPP-IV), a highly specific serine protease, with an IC50 of 4.6 nM.
DPP-IV-IN-1 (0.1 and 0.3 mg/kg, p.o.) reduces the increase in plasma glucose beginning 30 min after glucose loading, and significantly suppresses hyperglycemia at the dose of 0.3 mg/kg in a rat model of obesity and impaired glucose tolerance. The effect is based on its inhibitory effect on plasma DPP-IV activity[1].
[1]. Fukushima H, et al. Synthesis and structure-activity relationships of potent 4-fluoro-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors. Bioorg Med Chem. 2008 Apr 1;16(7):4093-106.