Sitagliptin-d4

• UNSPSC Description:

  Sitagliptin-d4 (MK-0431-d4) is deuterium labeled Sitagliptin. Sitagliptin (MK-0431) is a potent and orally active inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts[1][2].

• Target Antigen:

  Autophagy; Dipeptidyl Peptidase; Isotope-Labeled Compounds

• Type:

  Isotope-Labeled Compounds

• Related Pathways:

  Autophagy;Metabolic Enzyme/Protease;Others

• Field of Research:

  Metabolic Disease;Cancer

• Smiles:

  O=C(N1CC2=NN=C(C(F)(F)F)N2C([2H])([2H])C1([2H])[2H])C[C@H](N)CC3=CC(F)=C(F)C=C3F

• Molecular Weight:

  411.34

• References & Citations:

  [1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.|[2]Kim, S.J., et al., Dipeptidyl peptidase IV inhibition with MK0431 improves islet graft survival in diabetic NOD mice partially via T-cell modulation. Diabetes, 2009. 58(3): p. 641-51.|[3]Sangle, G.V., et al., Novel biological action of the dipeptidylpeptidase-IV inhibitor, sitagliptin, as a GLP-1 secretagogue. Endocrinology, 2012. 153(2): p. 564-73.|[4]Thomas, L., et al. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of action compared with other dipeptidyl peptidase-4 inhibitors. J Pharmacol Exp Ther. 2008 Apr;325(1):175-82.|[5]Kim, S.J., et al., Inhibition of dipeptidyl peptidase IV with sitagliptin (MK0431) prolongs islet graft survival in streptozotocin-induced diabetic mice. Diabetes, 2008. 57(5): p. 1331-9.|[6]Beconi, M.G., et al. Disposition of the dipeptidyl peptidase 4 inhibitor sitagliptin in rats and dogs. Drug Metab Dispos, 2007. 35(4): p. 525-32.

• Shipping Conditions:

  Room temperature

• Clinical Information:

  No Development Reported