The effect of limiglidol on the activity of dipeptidyl peptidase type 4 (DPP-4) in vitro and in vivo and on the morphological parameters of pancreatic islets have been investigated. Limiglidol exhibited dose-dependent inhibition of DPP-4 in vitro, but it was significantly lower compared to reference agents such as vildagliptin, sitagliptin, and diprotin A. After course of administration, limiglidol corrected blood glucose levels on the streptozotocin model of diabetes, but had no effect on the activity of DPP-4 and did not produce statistically significant increase in the specific number of endocrine β-cells.