Orally active, substrate-competitive, highly potent and selective dipeptidyl peptidase IV inhibitor with therapeutic efficacy against type 2 diabetes in vivo.
Teneligliptin is an orally active, substrate-competitive, highly potent and selective dipeptidyl peptidase IV inhibitor (IC50 in nM = 0.889/hrDPP-IV,1.75/human plasma, 1.35/rat plasma; 700- and 1500-fold selectivity over DPP-8 and DPP-9, respectively). Teneligliptin inhibits plasma DDP-IV activtiy (ED50 = 0.41mg/kg p.o. in Wistar rats) with therapeutic efficacy against type 2 diabetes in Zucker fa/fa rats in vivo (0.1-1 mg/kg p.o.).
Chronic hyperglycemia has deleterious effects on pancreatic β-cell function and survival in type 2 diabetes (T2D) due to the low expression level of endogenous antioxidants in the β-cells. Peroxiredoxin-3 (PRDX3) is a mitochondria specific H202 scavenger and protects the cell
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