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Teneligliptin

Catalog No. T37522 CAS 760937-92-6

Teneligliptin (MP-513) is a potent chemotype prolylthiazolidine-based DPP-4 inhibitor, which competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM.

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Teneligliptin, CAS 760937-92-6

Pack Size	Availability	Price/USD
5 mg	5 days	$ 30.00
10 mg	5 days	$ 44.00
1 mL * 10 mM (in DMSO)	5 days	$ 43.00

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Biological Description

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Description	Teneligliptin (MP-513) is a potent chemotype prolylthiazolidine-based DPP-4 inhibitor, which competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM.
Targets&IC50	DPP4:1 nM (IC50)
In vitro	Teneligliptin (MP-513) demonstrates concentration-dependent inhibition of DPP-4 enzymes across various contexts, with IC50 values of 0.889 nM for rhDPP-4, 1.75 nM for human plasma, and 1.35 nM for rat plasma. Enzyme inhibition kinetics, analyzed using Gly-Pro-MCA substrate and rhDPP-4, show Teneligliptin acts via a substrate-competitive mechanism. This is supported by residual sum of squares analyses, yielding 0.162 for competitive and 0.192 for non-competitive models, alongside calculated Ki, Km, and Vmax values of 0.406 nM, 24 μM, and 6.06 nmol/min, respectively. Furthermore, Teneligliptin effectively protects GLP-1(7-36)amide from degradation, evidenced by an IC50 of 2.92 nM.
In vivo	Oral administration of Teneligliptin (MP-513) to Wistar rats significantly inhibits plasma DPP-4 activity, achieving an ED50 of 0.41 mg/kg and maintaining this inhibition for 24 hours post-dose. When administered to Zucker fatty rats, Teneligliptin at doses of 0.1 mg/kg or higher enhances plasmaglucagon-like peptide-1 and insulin levels, curtails glucose levels during oral carbohydrate challenges up to 12 hours after a 1 mg/kg dose, and reduces triglyceride and free fatty acid levels after oral fat challenges. Continuous dosing over two weeks similarly decreases blood glucose, triglycerides, and free fatty acids under non-fasting conditions. Compared to Sitagliptin and Vildagliptin, with ED50 values of 27.3 and 12.8 mg/kg respectively, Teneligliptin shows a markedly higher potency in dose-dependent plasma DPP-4 inhibition. Additionally, Teneligliptin improves liver histopathology and reduces intrahepatic triglyceride levels in NAFLD model mice by downregulating genes involved in hepatic lipogenesis through AMPK activation.
Kinase Assay	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].

Molecular Weight	426.58
Formula	C22H30N6OS
CAS No.	760937-92-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 33.33 mg/mL (78.13 mM)

References and Literature

1. Fukuda-Tsuru S, et al. A novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor, teneligliptin, improves postprandial hyperglycemia and dyslipidemia after single and repeated administrations. Eur J Pharmacol. 2012 Dec 5;696(1-3):194-202. 2. Ideta T, et al. The Dipeptidyl Peptidase-4 Inhibitor Teneligliptin Attenuates Hepatic Lipogenesis via AMPK Activation in Non-Alcoholic Fatty Liver Disease Model Mice. Int J Mol Sci. 2015 Dec 8;16(12):29207-18.

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Teneligliptin 760937-92-6 inhibitor inhibit

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