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Biochem/physiol Actions
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.).
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| optical activity | [α]/D -28 to -36°, c = 0.5 in methanol |
| storage condition | desiccated |
| color | white to very dark gray |
| solubility | H2O: 2 mg/mL, clear |
| storage temp. | −20°C |
| SMILES string | CC1=NN(C(N2CCN(CC2)[C@@]3(CN[C@@H](C3)C(N4CSCC4)=O)[H])=C1)C5=CC=CC=C5.[xHBr].[yH2O] |
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