Teneligliptin

SKU: orb1692821

Description

Teneligliptin (MP-513) is a potent and selective DPP-4 inhibitor used in diabetes research. It is applied in both in vitro enzymatic assays and in vivo models to study mechanisms of glycemic control and metabolic disorders, including obesity and type 2 diabetes.

Research Area

Pharmacology & Drug Discovery, Protein Biochemistry

Key Properties

• CAS Number: 760937-92-6
• MW: 426.58
• Purity: 99.83% (May vary between batches)
• Formula: C₂₂H₃₀N₆OS
• SMILES: CC=1C=C(N(N1)C2=CC=CC=C2)N3CCN(CC3)[C@H]4C[C@@H](C(=O)N5CCSC5)NC4
• Target: DPP-4
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.69 mM);DMSO:20 mg/mL (46.88 mM)

Bioactivity

• Target IC50:
  GLP1(7-36) amide:2.92 nM|DPP4 (rat plasma):1.35 nM|DPP4 (human plasma):1.75 nM|DPP4 (human recombinant):0.406 nM (Ki)|DPP4 (human recombinant):24 μM (Km)|DPP4 (human recombinant):0.889 nM|DPP4 (human recombinant):6.06 nmol/min (Vmax)
  Read more...
• In Vivo:
  In Wistar rats, oral administration of Teneligliptin effectively inhibited plasma DPP-4 with an ED50 value of 0.41 mg/kg, and the inhibitory effect was sustained up to 24 hours after administration. Teneligliptin at a dose of 1 mg/kg significantly reduced triglyceride and free fatty acid fluctuations in an oral fat loading assay in Zucker rats. Zucker rats receiving Teneligliptin orally for two consecutive weeks demonstrated a reduction in blood glucose fluctuations in an oral glycemic load test, as well as a reduction in plasma triglyceride and free fatty acid levels in the non-fasting state. In addition, Teneligliptin improved hepatic histopathological features and reduced intrahepatic triglyceride levels in a mouse model of nonalcoholic fatty liver disease, which was associated with downregulation of hepatic lipid synthesis-related genes induced by AMPK activation.
  Read more...
• In Vitro:
  Teneligliptin inhibits DPP-4 enzyme in a concentration-dependent manner. The IC50 values of Teneligliptin on human recombinant DPP4 (rhDPP-4), human plasma and rat plasma were 0.889 nM, 1.75 nM and 1.35 nM, respectively. The kinetics of enzyme inhibition by Teneligliptin was investigated using Gly-Pro-MCA as the substrate and rhDPP-4 as the enzyme source, and the Ki, Km and Vmax values were 0.406 nM, 24 μM and 6.06 nmol/min, respectively. Teneligliptin inhibited the degradation of GLP-1(7-36)amide with an IC50 value of 2.92 nM.
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Teneligliptin, DPP4, DPP-4, MP513, MP-513

Compound Identifiers

PubChem CID

11949652