Sitagliptin-d6

• Description :

  Sitagliptin-d6 (MK-0431-d6) is deuterium labeled Sitagliptin (HY-13749) . Sitagliptin is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.

• Product Name Alternative :

  MK-0431-d6

• UNSPSC :

  12352005

• Target :

  Dipeptidyl Peptidase; Endogenous Metabolite; ERK; GLP Receptor; Isotope-Labeled Compounds; PKA

• Related Pathways :

  GPCR/G Protein; MAPK/ERK Pathway; Metabolic Enzyme/Protease; Others; Stem Cell/Wnt; TGF-beta/Smad

• Applications :

  COVID-19-immunoregulation

• Field of Research :

  Metabolic Disease

• Smiles :

  FC(F)(C1=NN=C2N1C([2H])([2H])C([2H])([2H])N(C(C[C@H](N)CC3=C(C=C(C(F)=C3)F)F)=O)C2([2H])[2H])F

• Molecular Formula :

  C16H9D6F6N5O

• Molecular Weight :

  413.35

• References & Citations :

  [1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]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.|[3]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.|[4]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.|[5]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.|[6]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.

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Isotope-Labeled Compounds

• Clinical Information :

  No Development Reported

• CAS Number :

  [1133211-99-0]