Sitagliptin (hydrochloride)
Sitagliptin (MK-0431) hydrochloride is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin hydrochloride 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 hydrochloride 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 hydrochloride shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin hydrochloride can be used for the study of 1-type and 2-type diabetes[1][2][3][4][5].
Product Specifications
CAS Number
486459-71-6
Product Name Alternative
MK-0431 (hydrochloride)
UNSPSC
12352005
Hazard Statement
H315-H319-H335
Target
Dipeptidyl Peptidase; Endogenous Metabolite; ERK; GLP Receptor; PKA
Related Pathways
GPCR/G Protein; MAPK/ERK Pathway; Metabolic Enzyme/Protease; 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.Cl
Molecular Formula
C16H16ClF6N5O
Molecular Weight
443.77
Precautions
P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P362+P364-P403+P233-P405-P501
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
DPP-4; ERK1; ERK2
Frequently Asked Questions
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