Teneligliptin CAS NO.760937-92-6

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Teneligliptin
UNII-28ZHI4CF9C
CS-0882

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ProName: Teneligliptin
CasNo: 760937-92-6
Molecular Formula: C22H30N6OS
Appearance: white powder
Application: Teneligliptin is a potent DPP-4 inhibi...
DeliveryTime: 4-15 days
PackAge: Aluminum foil bag packaging or as your...
Port: Shanghai Tianjin Guangzhou
ProductionCapacity: 50 Kilogram/Week
Purity: 98
Storage: Closed operation, local exhaust, wear ...
Transportation: by sea or air
LimitNum: 1 Kilogram

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Details

Delilintine biological activity

Description Teneligliptin is a potent DPP-4 inhibitor that competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 with IC50 of approximately 1 nM.

Related categories

Signaling Pathway >> Metabolic Enzymes / Proteases >> Dipeptidyl Peptidase

Research Area >> Metabolic Disease

Target

IC50: 1 nM (DPP4) [1]

In vitro studies Teneligliptin inhibits all these DPP-4 enzymes in a concentration-dependent manner. The IC50 of Teneligliptin for rhDPP-4, human plasma and rat plasma were 0.889, 1.75 and 1.35 nM, respectively. Gly-Pro-MCA was used as a substrate and rhDPP-4 was used as an enzyme source to study the kinetics of enzymatic inhibition of Teneligliptin. Graphs based on the Michaelis-Menten equation show that Teneligliptin inhibits DPP-4 in a substrate-competitive manner; the sum of squared residuals of the competitive model and the non-competitive model are 0.162 and 0.192, respectively. Ki, Km and Vmax values ??were 0.406 nM, 24 μM and 6.06 nmol / min. Teneligliptin inhibits the degradation of GLP-1 (7-36) amide with IC50 of 2.92 nM [1].

In vivo studies The oral administration of Teneligliptin in Wistar rats resulted in inhibition of plasma DPP-4 with an ED50 of 0.41 mg / kg. Plasma DPP-4 inhibition persisted even 24 hours after the administration of Teneligliptin. An oral carbohydrate load test in Zucker obese rats showed that Teneligliptin ≥ 0.1 mg / kg increased the maximum increase in plasma glucagon-like peptide-1 and insulin levels and reduced glucose excursion. This effect was observed 12 hours after the dose of 1 mg / kg. An oral fat load test in Zucker obese rats also showed that Teneligliptin at 1 mg / kg reduced triglyceride and free fatty acid drift. In Zucker obese rats, repeated administration of Teneligliptin for two weeks reduced glucose excursion in the oral carbohydrate load test and reduced plasma triglyceride and free fatty acid levels under non-fasting conditions. Oral administration of Teneligliptin inhibited DPP-4 in rat plasma in a dose-dependent manner. For Teneligliptin, the ED50 value was calculated to be 0.41 mg / kg, while the ED50 values ??of sitagliptin and vidagliptin were 27.3 and 12.8 mg / kg, respectively [1]. For the NAFLD model, tiganidine improves the histopathological manifestations of the liver and lowers triglyceride levels in mice, which is related to the down-regulation of liver adipogenesis-related genes caused by AMPK activation [2].

Kinase experiment DPP-4 inhibition assay was performed using 5ng of purified recombinant human DPP-4 (rhDPP-4), human plasma (diluted 20-fold with assay buffer; phosphate buffered saline (PBS) containing 0.003% Brij-35 solution) . Or rat plasma (diluted 10-fold with assay buffer) Gly-Pro-MCA as a chromogenic substrate, as described above, with a slight modification. DPP-4 inhibitors (Teneligliptin, Sitagliptin and Vildagliptin) were diluted with several concentrations of assay buffer. 20 μl of inhibitor solution, 20 μL of enzyme source and 20 μLGly-Pro-MCA (final concentration, 25 μM) were mixed with 140 μL or 160 μL of assay buffer to initiate the enzyme reaction. After 20 minutes (rhDPP-4) or 1 hour (plasma) at 37 ° C, the following 7-amino-4-methyl-coumarin (AMC) produced by Gly-Pro-MCA was measured using an automatic microplate reader. Fluorescence intensity: 360nm excitation and 465nm emission. The fluorescence intensity of AMC corresponds to DPP-4 activity [1].

Teneligliptin CAS NO.760937-92-6

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