Teneligliptin Hydrobromide is a DPP4 inhibitor with IC50 value of <1 nM. It is commonly used as an add on treatment when meformin is not achieving the expected glycemic goals.
Dipeptidylpeptidase 4 (DPP4) belongs to the S9b gene family of postproline serine peptidases. It acts mostly as a secreted membrane protein, mediating the degradation and inactivation of glucagon-like peptide (GLP)-1 and gastric inhibitory protein (GIP)[3]. Teneligliptin is a DPP4 inhibitor for the treatment of type 2 diabetes. Teneligliptin inhibits human plasma DPP-4 activity and recombinant human DPP-4 activity in a concentration-dependent manner with IC50 of 1.75 nM and 0.889 nM, respectively[4]. In human umbilical vein endothelial cells exposed to high glucose, teneligliptin (0.1, 1.0 and 3.0 µM) promoted the antioxidant response, reduced ROS levels and induced Nrf2-target genes messenger ribonucleic acid expression. It also improved proliferation rates, regulated the expression of cell-cycle inhibitors markers (P53, P21 and P27), and reduced proapoptotic genes (BAX and CASP3), while promoted BCL2 expression[5]. Teneligliptin effectively ameliorated the characteristics of metabolic abnormalities associated with postmenopausal obesity in ovariectomized (OVX) mice maintained on a high-fat diet[6].
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