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Trelagliptin(SYR-472)

Inquiry
  Post Date: Jan 09,2018
  Expiry Date: Jul 08,2018
  Detailed Description: Cas No. :1029877-94-8 Quantity: mass in stockKilograms
Specs:white powder
Price:negotiable USD Kilograms
Payment Method: T/T, Western Union,Moneygram and Bitcoin.
Description:

SYR-472 is a novel once-weekly oral DPP-4 inhibitor for type 2 diabetes, which could be a treatment option when clinicians seek to improve medication adherence by reducing the number of required administrations.

In study, The incidence of treatment-emergent adverse events in each SYR-472 group was similar to that in the placebo group. The most common adverse event was nasopharyngitis in all groups. No episodes of hypoglycaemia defined by investigator occurred with any treatment during the study. Once-weekly SYR-472 treatment produced clinically and statistically significant improvements in glycaemic control in patients with type 2 diabetes. It was well tolerated and might be a new treatment option for patients with this disease.


Application

Trelagliptin Succinate (SYR-472), a novel dipeptidyl peptidase-4 inhibitor, shows sustained efficacy by once-weekly dosing in type 2 diabetes patients.

In this study, we characterized in vitro properties of trelagliptin, which exhibited approximately 4- and 12-fold more potent inhibition against human dipeptidyl peptidase-4 than alogliptin and sitagliptin, respectively, and >10,000-fold selectivity over related proteases including dipeptidyl peptidase-8 and dipeptidyl peptidase-9. Kinetic analysis revealed reversible, competitive and slow-binding inhibition of dipeptidyl peptidase-4 by trelagliptin (t1/2 for dissociation ≈ 30 minutes).

X-ray diffraction data indicated a non-covalent interaction between dipeptidyl peptidase and trelagliptin. Taken together, potent dipeptidyl peptidase inhibition may partially contribute to sustained efficacy of trelagliptin.

  CAS Registry Number:

1029877-94-8

  Synonyms: ;Trelagliptin succinat;
  Molecular Formula: C22H26FN5O6
  Molecular Weight: 475.47000
  Molecular Structure: 1029877-94-8 Trelagliptin succinate

  Company: Hengyang Desen Biotechnology Co., Ltd.     [ China ]        
  Contact: ava
  Tel: 86-18908446905
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  Email: ava@ycgmp.com
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