Trelagliptin

Trelagliptin

Catalog Number:
L002368909APE
Mfr. No.:
APE-A3888
Price:
$228
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          Background

          Trelagliptin (SYR-472) is a selective inhibitor of DPP-4 and is developed for the treatment of type 2 diabetes mellitus (T2DM) [1].Dipeptidyl peptidase (DPP)-4 also known as adenosine deaminase complexing protein 2 or CD26 is an antigenic enzyme that expressed on the surface of most cell types and plays an important role in regulating immune system, signal transduction and apoptosis [2, 3].Trelagliptin (SYR-472) is a potent DPP-4 inhibitor and can be administered once weekly which unlike its other class approved agents that be taken once daily [1]. In Japan, clinical trials had been conducted to detect the effectiveness of Trelagliptin by comparing with the approved medicine—alogliptin and it was shown that Trelagliptin once-weekly exhibited similar efficacy and safety to alogliptin once daily, which indicated that Trelagliptin could be a useful new antidiabetes drug that needs to be given once a week [2].Trelagliptin (SYR-472) has been used in phase 2 and phase 3 clinical trials for the treatment of patients with T2DM showed similar efficacy and safety to alogliptin once daily and produced clinically and statistically significant improvements in glycaemic control with well tolerated in Japan [2, 3].

          [1]. McKeage, K., Trelagliptin: First Global Approval. Drugs, 2015. 75(10): p. 1161-4.
          [2]. Inagaki, N., et al., Once-weekly trelagliptin versus daily alogliptin in Japanese patients with type 2 diabetes: a randomised, double-blind, phase 3, non-inferiority study. Lancet Diabetes Endocrinol, 2015. 3(3): p. 191-7.
          [3]. Inagaki, N., et al., SYR-472, a novel once-weekly dipeptidyl peptidase-4 (DPP-4) inhibitor, in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial. Lancet Diabetes Endocrinol, 2014. 2(2): p. 125-32.

      • Properties
        • Alternative Name
          SYR-472,SYR472,SYR 472,Trelagliptin; 2-[[6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]-4-fluorobenzonitrile
          CAS Number
          865759-25-7
          Molecular Formula
          C18H20FN5O2
          Molecular Weight
          357.38
          Appearance
          A solid
          Purity
          99.66%
          Solubility
          ≥11.6 mg/mL in DMSO; ≥3.68 mg/mL in EtOH with gentle warming and ultrasonic; ≥93.8 mg/mL in H2O
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Ryeon Heo, Mi Seon Seo, et al. "The anti-diabetic drug trelagliptin induces vasodilation via activation of Kv channels and SERCA pumps." Life Sci. 2021 Oct 15;283:119868. PMID:34358551

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