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 phosphate monohydrate

Sitagliptin phosphate monohydrate  (Synonyms: MK-0431 phosphate monohydrate)

Cat. No.: HY-13749B Purity: 99.83%
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Sitagliptin (MK-0431) phosphate monohydrate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate monohydrate 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 phosphate monohydrate 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 phosphate monohydrate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate monohydrate 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. : 654671-77-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
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Customer Review

Based on 30 publication(s) in Google Scholar

Other Forms of Sitagliptin phosphate monohydrate:

Sitagliptin phosphate monohydrate Related Antibodies

Top Publications Citing Use of Products

30 Publications Citing Use of MCE Sitagliptin phosphate monohydrate

In Vivo Efficacy Study
Histological Imaging/Staining
IF
RT-PCR

    Sitagliptin phosphate monohydrate 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 phosphate monohydrate 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 phosphate monohydrate 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 phosphate monohydrate 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 phosphate monohydrate 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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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Sitagliptin (MK-0431) phosphate monohydrate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate monohydrate 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 phosphate monohydrate 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 phosphate monohydrate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate monohydrate can be used for the study of 1-type and 2-type diabetes[1][2][3][4][5].

    IC50 & Target

    DPP-4

    19 nM (IC50)

    In Vitro

    Sitagliptin phosphate exhibits a potent inhibitory effect on DPP-4 with IC50 of 19 nM from Caco-2 cell extracts[1]. Sitagliptin reduces in vitro migration of isolated splenic CD4 T-cells through a pathway involving cAMP/PKA/Rac1 activation[2]. A recent study demonstrates that sitagliptin exerts a novel, direct action in order to stimulate GLP-1 secretion by the intestinal L cell through a DPP-4-independent, protein kinase A- and MEK-ERK1/2-dependent pathway. It therefore reduces the effect of autoimmunity on graft survival[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Sitagliptin phosphate monohydrate Related Antibodies
    In Vivo

    In vivo, the ED50 value of sitagliptin phosphate for inhibition of plasma DPP-4 activity is calculated to be 2.3 mg/kg 7 hour postdose and 30 mg/kg 24 hour postdose in freely fed Han-Wistar rats[1]. The streptozotocin-induced type 1 diabetes mouse model exhibits elevated DPP-4 levels in the plasma that can be substantially inhibited in mice on an Sitagliptin phosphate diet. This is achieved by a positive effect on the regulation of hyperglycemia, potentially through prolongation of islet graft survival[4]. The plasma clearance and volume of distribution of Sitagliptin phosphate are higher in rats (40-48 mL/min/kg, 7-9 L/kg) than in dogs (9 mL/min/kg, 3 L/kg); and its half-life is shorter in rats,2 hours compared with 4 hours in dogs[5].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    523.32

    Formula

    C16H20F6N5O6P
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    H2O : ≥ 33 mg/mL (63.06 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9109 mL 9.5544 mL 19.1088 mL
    5 mM 0.3822 mL 1.9109 mL 3.8218 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 50 mg/mL (95.54 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.83%

    SDS (394 KB)

    COA (253 KB) HNMR (260 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    CD4T-cells are plated on membrane inserts in serum-free RPMI 1640, and cell migration is assayed using Transwell chambers (Corning), in the presence or absence of purified porcine kidney DPP-4 (32.1 units/mg; 100 mU/mL final concentration) and DPP-4 inhibitor (100 μM). After 1 hour, cells on the upper surface are removed mechanically, and cells that have migrated into the lower compartment are counted. The extent of migration is expressed relative to the control sample.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice: Overnight fasted C57BL/6J mice are challenged 45 min after compound administration with an oral glucose load (2 g/kg). Blood samples for glucose measurement are obtained by tail bleed predose and at serial time points after the glucose load. To evaluate the duration of the effect on glucose tolerance, vehicle or DPP-4 inhibitors are administered 16 h before the glucose challenge.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O 1 mM 1.9109 mL 9.5544 mL 19.1088 mL 47.7719 mL
    5 mM 0.3822 mL 1.9109 mL 3.8218 mL 9.5544 mL
    10 mM 0.1911 mL 0.9554 mL 1.9109 mL 4.7772 mL
    15 mM 0.1274 mL 0.6370 mL 1.2739 mL 3.1848 mL
    20 mM 0.0955 mL 0.4777 mL 0.9554 mL 2.3886 mL
    25 mM 0.0764 mL 0.3822 mL 0.7644 mL 1.9109 mL
    30 mM 0.0637 mL 0.3185 mL 0.6370 mL 1.5924 mL
    40 mM 0.0478 mL 0.2389 mL 0.4777 mL 1.1943 mL
    50 mM 0.0382 mL 0.1911 mL 0.3822 mL 0.9554 mL
    60 mM 0.0318 mL 0.1592 mL 0.3185 mL 0.7962 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Sitagliptin phosphate monohydrate Related Classifications

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    • Do most proteins show cross-species activity?

      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:

    Sitagliptin phosphate654671-77-9MK-0431 phosphateDipeptidyl PeptidaseGLP ReceptorEndogenous MetabolitePKAERKDPPProtein kinase AExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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