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Cat. No.: HY-13749E

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Sitagliptin hydrochloride

(Synonyms: MK-0431 hydrochloride)

31 Cited Publications

고객리뷰

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.

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CAS No.: 486459-71-6
화학식: C₁₆H₁₆ClF₆N₅O
분자량:443.77

보관:

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

Data Sheet (243 KB)

Sitagliptin hydrochloride Chemical Structure

CAS No.: 486459-71-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
Chemical Information
Publications (31)
순도&문서
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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

All Endogenous Metabolite Isoforms :

All PKA Isoforms :

All Dipeptidyl Peptidase Isoforms :

All ERK Isoforms :

Chemical Information

CAS No. 486459-71-6
분자량 443.77
화학식 C₁₆H₁₆ClF₆N₅O
SMILES

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

MK-0431 hydrochloride
선적

Room temperature in continental US; may vary elsewhere.
보관

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

Publications (31)

All In Vivo Efficacy StudyHistological Imaging/StainingIFRT-PCR

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Journal Impact Factor

J Adv Res

Hippocampal dipeptidyl peptidase 9 bidirectionally regulates memory associated with synaptic plasticity. [Abstract]

2025 Aug:74:225-236. PMID: 39369958
Gut Microbes

Dual-source DPP4 drives intestinal fibrosis in Crohn's disease: synergistic therapeutic targeting of host and microbiota pathways. [Abstract]

2025 Dec 31;17(1):2593119. PMID: 41334589

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.
J Nanobiotechnology

Metal-organic-framework-based sitagliptin-release platform for multieffective radiation-induced intestinal injury targeting therapy and intestinal flora protective capabilities. [Abstract]

2024 Oct 16;22(1):631. PMID: 39415273
Cell Death Dis

Sitagliptin activates the p62-Keap1-Nrf2 signalling pathway to alleviate oxidative stress and excessive autophagy in severe acute pancreatitis-related acute lung injury. [Abstract]

2021 Oct 11;12(10):928. PMID: 34635643
Int J Biol Macromol

Comprehending the mechanism of catechins against α-glucosidase by multispectral data and their antidiabetic effects in vivo. [Abstract]

2025 Jun 6;318(Pt 1):145051. PMID: 40484085
J Ethnopharmacol

Eucommia alleviates high fat diet-induced MASLD via the F. prausnitzii/butyrate/GPR43/GLP-1 signaling. [Abstract]

2025 Sep 9;355(Pt A):120587. PMID: 40935212
Biochem Pharmacol

Melatonin protects HT-22 cells against palmitic acid-induced glucolipid metabolic dysfunction and cell injuries: Involved in the regulation of synaptic plasticity and circadian rhythms. [Abstract]

2023 Nov:217:115846. PMID: 37804870
Life Metab

Development of cyclopeptide inhibitors specifically disrupting FXR-coactivator interaction in the intestine as a novel therapeutic strategy for MASH. [Abstract]

2025 Feb 8;4(2):loaf004. PMID: 40225300
World J Diabetes

Pig bile powder maintains blood glucose homeostasis by promoting glucagon-like peptide-1 secretion via inhibiting farnesoid X receptor. [Abstract]

2025 Jun 15;16(6):103616. PMID: 40548276
Biochim Biophys Acta Mol Basis Dis

Dapagliflozin attenuates AKI to CKD transition in diabetes by activating SIRT3/PGC1-α signaling and alleviating aberrant metabolic reprogramming. [Abstract]

2024 Oct;1870(7):167433. PMID: 39067538
Sci Rep

The In Vitro Biotransformation of the Fusion Protein Tetranectin-Apolipoprotein A1. [Abstract]

2019 Mar 11;9(1):4074. PMID: 30858459
Mol Oncol

Therapeutic strategies for MMAE-resistant bladder cancer through DPP4 inhibition. [Abstract]

2025 Dec 21. PMID: 41422479
iScience

Non-canonical function of DPP4 promotes cognitive impairment through ERp29-associated mitochondrial calcium overload in diabetes. [Abstract]

2023 Feb 27;26(3):106271. PMID: 36936785
Nutrition

Lactobacillus plantarum NCHBL-004 modulates high-fat diet-induced weight gain and enhances GLP-1 production for blood glucose regulation. [Abstract]

2024 Dec:128:112565. PMID: 39326237
J Sep Sci

High-throughput bioanalysis of sitagliptin in plasma using direct analysis in real time mass spectrometry and its application in the pharmacokinetic study thereof. [Abstract]

2022 Jan;45(2):631-637. PMID: 34709732
BMC Pharmacol Toxicol

Repurposing DPP-4 inhibitors as anticancer agents in KRAS-mutated pancreatic ductal adenocarcinoma. [Abstract]

2025 Dec 8;26(1):208. PMID: 41361888
Exp Cell Res

SOX9 promotes hypoxic pulmonary hypertension through stabilization of DPP4 in pulmonary artery smooth muscle cells. [Abstract]

2024 Sep 12;442(2):114254. PMID: 39276964
Front Oncol

Antidiabetic DPP-4 Inhibitors Reprogram Tumor Microenvironment That Facilitates Murine Breast Cancer Metastasis Through Interaction With Cancer Cells via a ROS-NF-кB-NLRP3 Axis. [Abstract]

2021 Sep 24:11:728047. PMID: 34631556
Tissue Cell

Saligenin restores insulin responsiveness in lipotoxic myotubes through L-cell-derived GLP-1 via ER stress-autophagy modulation. [Abstract]

2026 Jun 17:103:103704. PMID: 42320358
3 Biotech

Neuroprotective effects of DPP-4 inhibitors sitagliptin and vildagliptin in Parkinson's disease via autophagy modulation. [Abstract]

2026 Apr;16(4):146. PMID: 41853215
Nutr Neurosci

High-fat diet induces depression-like behaviour in mice associated with changes in microbiome, neuropeptide Y, and brain metabolome. [Abstract]

2019 Dec;22(12):877-893. PMID: 29697017
Korean J Physiol Pharmacol

Sitagliptin attenuates endothelial dysfunction independent of its blood glucose controlling effect. [Abstract]

2021 Sep 1;25(5):425-437. PMID: 34448460
Arch Oral Biol

Sitagliptin regulates the AMPK/NF-κB signaling pathway to alleviate lipopolysaccharide-induced inflammatory responses and promote osteogenic differentiation in rat bone marrow mesenchymal stem cells. [Abstract]

2025 Jul:175:106253. PMID: 40215713
Neurol Res

Sitagliptin rescues memory deficits in Parkinsonian rats via upregulating BDNF to prevent neuron and dendritic spine loss. [Abstract]

2018 Sep;40(9):736-743. PMID: 29781786
bioRxiv

Characterizing the SASP-Dependent Paracrine Spreading of Senescence Between Human Brain Cell Types. [Abstract]

2026 Feb 12:2026.02.10.705129. PMID: 41726875
Orebro University

2024.
Research Square Preprint

2024 Apr 25.
bioRxiv

2023 Nov 4.
Biomed Pharmacother

Sitagliptin inhibits the survival, stemness and autophagy of glioma cells, and enhances temozolomide cytotoxicity. [Abstract]

2023 Jun:162:114555. PMID: 36966667
Oxid Med Cell Longev

Sitagliptin Alleviates Radiation-Induced Intestinal Injury by Activating NRF2-Antioxidant Axis, Mitigating NLRP3 Inf--lammasome Activation, and Reversing Gut Microbiota Disorder. [Abstract]

2022 May 17;2022:2586305. PMID: 35620578
Oxid Med Cell Longev

DPP4 Inhibitor Attenuates Severe Acute Pancreatitis-Associated Intestinal Inflammation via Nrf2 Signaling. [Abstract]

2019 Nov 15:2019:6181754. PMID: 31827684

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (243 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Calculators

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration Concentration

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Volume Volume

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Molecular Weight Molecular Weight

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Concentration _(start) Concentration _(start)

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Volume _(start) Volume _(start)

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×

Volume _(final) Volume _(final)

Keywords

Sitagliptin hydrochloride

31 Cited Publications

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Biological Activity
- 제품 설명
- IC₅₀ & Target
Chemical Information
Publications (31)
순도&문서

1/16
1/16

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.