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Sitagliptin hydrochloride

(Synonyms: MK-0431 hydrochloride)
31 Cited Publications
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Based on 31 publication(s) in Google Scholar

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.

For research use only. We do not sell to patients.

  • CAS No.: 486459-71-6
  • Formula: C16H16ClF6N5O
  • Molecular Weight:443.77
  • Storage:

    Please store the product under the recommended conditions in the Certificate of Analysis.

  • Sitagliptin hydrochloride Chemical Structure
    Sitagliptin hydrochloride Chemical Structure
  • Experimental Validation Results for Sitagliptin hydrochloride
  • Experimental Validation Results for Sitagliptin hydrochloride
  • Experimental Validation Results for Sitagliptin hydrochloride
  • Experimental Validation Results for Sitagliptin hydrochloride
  • Experimental Validation Results for Sitagliptin hydrochloride
CAS No.: 486459-71-6
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In Vivo Efficacy StudyHistological Imaging/StainingIFRT-PCR
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  • Histological Imaging/Staining
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  • Sitagliptin hydrochloride Chemical Structure
    Sitagliptin hydrochloride Chemical Structure
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    Sitagliptin hydrochloride purchased from MedChemExpress. Usage Cited in: Gut Microbes. 2025 Dec 31;17(1):2593119. [Abstract]

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • Sitagliptin hydrochloride