2. Metabolic Enzyme/Protease GPCR/G Protein TGF-beta/Smad Stem Cell/Wnt MAPK/ERK Pathway
  3. Dipeptidyl Peptidase GLP Receptor Endogenous Metabolite PKA ERK
  4. Sitagliptin hydrochloride

Sitagliptin hydrochloride  (Synonyms: MK-0431 hydrochloride)

Cat. No.: HY-13749E
Handling Instructions Technical Support

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.

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CAS No. : 486459-71-6

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30 Publications Citing Use of MCE Sitagliptin hydrochloride

In Vivo Efficacy Study
Histological Imaging/Staining
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RT-PCR

    Sitagliptin hydrochloride purchased from MedChemExpress. Usage Cited in: Gut Microbes. 2025 Dec 31;17(1):2593119.  [Abstract]

    Colon length quantification in the DSS group (n = 6) and DSS + DPP4i group (n = 6). Mice received three cycles of 1.5% DSS (7 days per cycle), each followed by a 14-day recovery phase. The DPP4 inhibitor sitagliptin was administered via oral gavage for 21 days during the final cycle of the experiment.

    Sitagliptin hydrochloride purchased from MedChemExpress. Usage Cited in: Gut Microbes. 2025 Dec 31;17(1):2593119.  [Abstract]

    Representative H&E-stained colon sections (left) and histologic inflammation scores (right). Mice received three cycles of 1.5% DSS (7 days per cycle), each followed by a 14-day recovery phase. The DPP4 inhibitor sitagliptin was administered via oral gavage for 21 days during the final cycle of the experiment.

    Sitagliptin hydrochloride purchased from MedChemExpress. Usage Cited in: Gut Microbes. 2025 Dec 31;17(1):2593119.  [Abstract]

    Representative Masson’s trichrome-stained colon sections and quantification of collagen volume fraction. Mice received three cycles of 1.5% DSS (7 days per cycle), each followed by a 14-day recovery phase. The DPP4 inhibitor sitagliptin was administered via oral gavage for 21 days during the final cycle of the experiment.

    Sitagliptin hydrochloride purchased from MedChemExpress. Usage Cited in: Gut Microbes. 2025 Dec 31;17(1):2593119.  [Abstract]

    Immunofluorescence images and quantification of α-SMA⁺ fibrotic thickness in the muscularis propria. Mice received three cycles of 1.5% DSS (7 days per cycle), each followed by a 14-day recovery phase. The DPP4 inhibitor sitagliptin was administered via oral gavage for 21 days during the final cycle of the experiment.

    Sitagliptin hydrochloride purchased from MedChemExpress. Usage Cited in: Gut Microbes. 2025 Dec 31;17(1):2593119.  [Abstract]

    RT-qPCR analysis of mRNA levels in colon tissues. Mice received three cycles of 1.5% DSS (7 days per cycle), each followed by a 14-day recovery phase. The DPP4 inhibitor sitagliptin was administered via oral gavage for 21 days during the final cycle of the experiment.

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    DPP-1 DPP-2 DPP-4 DPP-8 DPP-9

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    Human Endogenous Metabolite Microbial Metabolite

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    PKA PKAR PKACα

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    ERK ERK1 ERK2 ERK5 ERK8

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    Description

    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].

    IC50 & Target[1][3]

    DPP-4

    19 nM (IC50)

    ERK1

     

    ERK2

     

    Molecular Weight

    443.77

    Formula

    C16H16ClF6N5O
    CAS No.
    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
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    Sitagliptin hydrochloride Related Classifications

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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Sitagliptin486459-71-6MK-0431MK0431MK 0431Dipeptidyl PeptidaseGLP ReceptorEndogenous MetabolitePKAERKDPPProtein kinase AExtracellular signal regulated kinasesPharmacokineticsMetabolismDPP-IV InhibitionGLP-1 SecretionIslet Graft SurvivalInhibitorinhibitorinhibit

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