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Sitagliptin

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

Sitagliptin (MK-0431) 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.

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  • Pureza: 99.94%
  • No. CAS: 486460-32-6
  • Fòrmula: C16H15F6N5O
  • Peso molecular:407.31
  • Almacenamiento:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 2 years , -20°C, 1 year
  • Sitagliptin Chemical Structure
    Sitagliptin Chemical Structure
  • Experimental Validation Results for Sitagliptin
  • Experimental Validation Results for Sitagliptin
  • Experimental Validation Results for Sitagliptin
  • Experimental Validation Results for Sitagliptin
  • Experimental Validation Results for Sitagliptin
No. CAS: 486460-32-6
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In Vivo Efficacy StudyHistological Imaging/StainingIFRT-PCR
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  • Sitagliptin Chemical Structure
    Sitagliptin Chemical Structure
    1/16
  • 1/16

    Sitagliptin 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 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 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 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 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