Teneligliptin (MP-513) is a novel dipeptidyl peptidase 4 (DPP IV) inhibitor for the treatment of type 2 diabetes mellitus with hypoglycemic activity for the study of obesity and diabetes.

DPP4 (human recombinant):0.406 nM (Ki), DPP4 (human recombinant):24 μM (Km), DPP4 (rat plasma):1.35 nM, DPP4 (human recombinant):0.889 nM, DPP4 (human recombinant):6.06 nmol/min (Vmax), DPP4 (human plasma):1.75 nM, GLP1(7-36) amide:2.92 nM

DPP-4 inhibition assay is carried out using either 5 ng purified recombinant human DPP-4 (rhDPP-4), human plasma (20-fold diluted with assay buffer; phosphate-buffered saline (PBS) containing 0.003% Brij-35 solution), or rat plasma (10-fold diluted with assay buffer) Gly-Pro-MCA as a chromogenic substrate as described previously with slight modifications. DPP-4 inhibitors (Teneligliptin, Sitagliptin, and Vildagliptin) are diluted with assay buffer at several concentrations. Twenty microliters of inhibitor solution, 20 μL of the enzyme source, and 20 μL of Gly-Pro-MCA (final concentration, 25 μM) are mixed with 140 μL or 160 μL of assay buffer to initiate the enzyme reaction. After 20 min (rhDPP-4) or 1 h (plasma) at 37°C, the fluorescence intensity of 7-amino-4-methyl-coumarin (AMC) generated from Gly-Pro-MCA is measured using an automated microplate reader at 360 nm excitation and 465 nm emission. The fluorescence intensity of AMC corresponded to DPP-4 activity[1].