DPP-4 inhibitor 1

DPP-4 inhibitor 1 (compound 5) is a potent and long acting Dipeptidyl peptidase-4 (DPP-4) inhibitor for t treatment of T2DM, with a KD of 0.177 nM[1].

Signaling Pathways >> Metabolic Enzyme/Protease >> Dipeptidyl Peptidase

Research Areas >> Metabolic Disease

KD: 0.177 nM (DPP-4)[1].

A single-dose oral administration of DPP-4 inhibitor 1 (compound 5) (3 mg/kg) inhibits >80% of DPP-4 activity for more than 7 days in diabetic mice[1]. Administration of DPP-4 inhibitor 1 (compound 5) (3 and 10 mg/kg, p.o., qw for 8 weeks) causes significant reductions in fasting blood glucose (FBG) levels, and the average reduction during the entire treatment period is 24.7 and 33.1%, respectively. Chronic administration of DPP-4 inhibitor 1 (compound 5) (10 mg/kg/week) also significantly improves the glucose tolerance of the diabetic mice[1]. Animal Model: ICR mice[1]. Dosage: 0.3, 3, 10 mg/kg. Administration: Oral, once. Result: Resulted in a time- and dose-dependent inhibition of plasma DPP-4 activity. The active GLP-1 and insulin level were significantly increased compared with the vehicle control. Animal Model: Genetic-type 2 diabetes animal models in db/db Mice[1]. Dosage: 3 and 10 mg/kg. Administration: Oral administration once a week, for 8 weeks. Result: Caused significant reductions in fasting blood glucose (FBG) levels. Improved the glucose tolerance of the diabetic mice significantly.

[1]. Li S, et al. Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. J Med Chem. 2019 Feb 1.