Sitagliptin (Standard)

• Description:

  Sitagliptin (Standard) is the analytical standard of Sitagliptin (HY-13749) . This product is intended for research and analytical applications. 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 (Standard)

• UNSPSC:

  12352100

• Target:

  Dipeptidyl Peptidase; Endogenous Metabolite; ERK; GLP Receptor; PKA; Reference Standards

• Related Pathways:

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

• Field of Research:

  Metabolic Disease

• Smiles:

  O=C(N1CC2=NN=C(C(F)(F)F)N2CC1)C[C@H](N)CC3=CC(F)=C(F)C=C3F

• Molecular Formula:

  C16H15F6N5O

• Molecular Weight:

  407.31

• References & Citations:

  [1]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.|[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]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.|[5]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

• Scientific Category:

  Reference Standards

• Clinical Information:

  Launched

• CAS Number:

  [486460-32-6]