Products for Research Use Only
RegisterLogin

Sitagliptin (phosphate)

CAT: 0804-HY-13749A-01Size: 100 mgDry Ice: NoHazardous: No
Product image 1
1 / 1
CAT#:0804-HY-13749A-01Size:100 mg
Selected
24/48H Stock Items & 2 to 6 Weeks non Stock Items.
Quick Request Actions
Description
Sitagliptin (MK-0431) phosphate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate 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 phosphate 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 phosphate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate can be used for the study of 1-type and 2-type diabetes[1][2][3][4][5].
CAS Number
654671-78-0
Product Name Alternative
MK-0431 (phosphate)
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Dipeptidyl Peptidase; Endogenous Metabolite; ERK; GLP Receptor; PKA
Type
Reference compound
Related Pathways
GPCR/G Protein; MAPK/ERK Pathway; Metabolic Enzyme/Protease; Stem Cell/Wnt; TGF-beta/Smad
Applications
COVID-19-immunoregulation
Field of Research
Metabolic Disease
Assay Protocol
https://www.medchemexpress.com/sitagliptin-phosphate.html
Purity
99.64
Solubility
DMSO : 100 mg/mL (ultrasonic) |H2O : 50 mg/mL (ultrasonic)
Smiles
O=C(N1CC2=NN=C(C(F)(F)F)N2CC1)C[C@H](N)CC3=CC(F)=C(F)C=C3F.O=P(O)(O)O
Molecular Formula
C16H18F6N5O5P
Molecular Weight
505.31
Precautions
H302, H315, H319, H335
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-ylm ethyl) -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 acti|[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 glucagon-like peptide-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
Storage Conditions
4°C (Powder, sealed storage, away from moisture and light)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
DPP-4

Related Products

CatalogName
HY-13749AS-01Sitagliptin-d4 (phosphate)
HY-13749-01Sitagliptin
HY-13749S3Sitagliptin-d6
HY-13749ESitagliptin (hydrochloride)
HY-13749R-01Sitagliptin (Standard)
HY-147401-01Sitagliptin fenilalanil
HY-13749D-01(Rac) -Sitagliptin
HY-13749S2Sitagliptin-d4
HY-Z3877-01Sitagliptin impurity 1
HY-131250-01N-Boc-Sitagliptin

Alternative Products

CatalogName
C3966-250Sitagliptin (phosphate)
MBS3616294-01Sitagliptin phosphate
A4036-5.1Sitagliptin phosphate monohydrate

Popular Products