Teneligliptin

Teneligliptin

Teneligliptin

Min.Order / FOB Price:Get Latest Price

1 Kilogram

Negotiable

  • Min.Order :1 Kilogram
  • Purity: 98
  • Payment Terms : T/T,Other

Keywords

Teneligliptin UNII-28ZHI4CF9C CS-0882

Quick Details

  • Appearance:white powder
  • Application: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.
  • PackAge:Aluminum foil bag packaging or as your request
  • ProductionCapacity:50|Kilogram|Week
  • Storage:Closed operation, local exhaust, wear goggles, gloves and protective clothing when working.
  • Transportation:by sea or air

Superiority:

1,Best Quality:

Our products have exported to Germany, Spain, UK, USA, Australia, Middle East, and so on other countries, and we have got very good feedback from our customers.so you can trust us.

2, Payment method: for example T/T, Westerm Union,other

3, Excellent Service: Best service and after-sales service to all clients.

   1)We will ship the goods within 5days after get your payments.If you want to cancel or change order, please tell me within 24hours after you finish the payment..

   2)We will ship the goods that you order from us by DHL, UPS, TNT and EUB.We will decided to choose which courier depend on different countries.To find the best way to delivery the goods for you.

   3)As usual you can get the goods with in 4-7days.If the goods were lost or not received for other reasons, please contact us immediately.

4,Fast and safe delivery:

Sample Order : As usual you can get the goods within 4-7days. We can send it via HKems, HK Air Post, DHL or other methods.

We have a professional and stable logistics, and we can deliver the package smoothly around 3 to 5 days.

Bulk Order: Shipped via sea or air, it's according to your requirement, delivery time is 7-15days after payment.

 

If you have any other questions to consult me,please not hesitate to contact me any times.

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].

View All
Visit Store

You Might Also Like

Related Searches

Contact Supplier

Confirm to collect the product to my collection?

OKCancel

About|Contact|Cas|Product Name|Molecular|Country|Encyclopedia

Message|New Cas|MSDS|Service|Advertisement|CAS DataBase|Article Data|Manufacturers | Chemical Catalog

©2008 LookChem.com,License: ICP

NO.:Zhejiang16009103

complaints:service@lookchem.com Desktop View