Products for Research Use Only
RegisterLogin

Sitagliptin-d4

CAT: 0804-HY-13749S2Size: 1 EachDry Ice: NoHazardous: No
Product image 1
1 / 1
CAT#:0804-HY-13749S2Size:1 Each
Selected
24/48H Stock Items & 2 to 6 Weeks non Stock Items.
Quick Request Actions
Description
Sitagliptin-d4 (MK-0431-d4) is deuterium labeled Sitagliptin. 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-d4
UNSPSC
12352005
Target
Dipeptidyl Peptidase; Endogenous Metabolite; ERK; GLP Receptor; Isotope-Labeled Compounds; PKA
Type
Isotope-Labeled Compounds
Related Pathways
GPCR/G Protein; MAPK/ERK Pathway; Metabolic Enzyme/Protease; Others; Stem Cell/Wnt; TGF-beta/Smad
Applications
Metabolism-sugar/lipid metabolism
Field of Research
Metabolic Disease
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 Formula
C16H11D4F6N5O
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
Scientific Category
Isotope-Labeled Compounds
Clinical Information
No Development Reported

Related Products

CatalogName
HY-13749-01Sitagliptin
HY-13749S3Sitagliptin-d6
HY-13749R-01Sitagliptin (Standard)
HY-147401-01Sitagliptin fenilalanil
HY-13749ESitagliptin (hydrochloride)
HY-13749A-01Sitagliptin (phosphate)
HY-13749D-01(Rac) -Sitagliptin
HY-Z3877-01Sitagliptin impurity 1
HY-13749AR-01Sitagliptin (phosphate) (Standard)
HY-131250-01N-Boc-Sitagliptin

Alternative Products

CatalogName
RM-S200788-01Sitagliptin-D4
sc-220106Sitagliptin-d4 Phosphate
RM-S200792-01(R) -Sitagliptin-D4
CS-ZB-09050Rac Sitagliptin D4
CS-O-02775Sitagliptin-d4 Hydrochloride
CS-O-46149Formyl sitagliptin d4
ESS0305-01Sitagliptin-D4 HCl
sc-473139Sitagliptin Triazecine Analog-D4
TRC-S491027-50MGent-Sitagliptin-d4 Phosphate
RM-S200836-01N-Nitroso Sitagliptin-D4

Popular Products