Trelagliptin-13C, d3

Trelagliptin-13C, d3 is a deuterated labeled Trelagliptin[1]. Trelagliptin (SYR-472) is a potent, orally active and highly selective DPP-4 inhibitor with an IC50 of 4 nM. Trelagliptin succinate improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM) [2].

Product Specifications

CAS Number

[2707203-34-5]

Product Name Alternative

SYR-472-13C, d3

UNSPSC

12352005

Target

Dipeptidyl Peptidase; Isotope-Labeled Compounds

Type

Isotope-Labeled Compounds

Related Pathways

Metabolic Enzyme/Protease; Others

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease

Smiles

N#CC1=CC=C(F)C=C1CN(C(N2[13C]([2H])([2H])[2H])=O)C(N3C[C@H](N)CCC3)=CC2=O

Molecular Formula

C17 13CH17D3FN5O2

Molecular Weight

361.39

References & Citations

[1]Bhumika D Patel, et al. Recent approaches to medicinal chemistry and therapeutic potential of dipeptidyl peptidase-4 (DPP-4) inhibitors. Eur J Med Chem. 2014 Mar 3;74:574-605.|[2]Charles E Grimshaw, et al. Trelagliptin (SYR-472, Zafatek), Novel Once-Weekly Treatment for Type 2 Diabetes, Inhibits Dipeptidyl Peptidase-4 (DPP-4) via a Non-Covalent Mechanism. PLoS One. 2016 Jun 21;11 (6) :e0157509.|[3]Shiliang Li, et al. Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. J Med Chem. 2019 Mar 14;62 (5) :2348-2361.|[4]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53 (2) :211-216.