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

Sitagliptin phosphate  (Synonyms: MK-0431 phosphate)

製品番号: HY-13749A 純度: 99.88%
COA 取扱説明書 Technical Support

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

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CAS 番号 : 654671-78-0

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カスタマーレビュー

Based on 30 publication(s) in Google Scholar

Other Forms of Sitagliptin phosphate:

Sitagliptin phosphate 関連抗体

Top Publications Citing Use of Products

顧客検証

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

    Sitagliptin phosphate 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 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 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 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 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.

    Dipeptidyl Peptidase アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    DPP-1 DPP-2 DPP-4 DPP-8 DPP-9

    Endogenous Metabolite アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    Human Endogenous Metabolite Microbial Metabolite

    PKA アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    PKA PKAR PKACα

    ERK アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    ERK ERK1 ERK2 ERK5 ERK8

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    製品説明

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

    IC50 & Target

    DPP-4

     

    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    11 3
    Compound: MK-0431
    Inhibition of human DPP8 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
    Inhibition of human DPP8 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
    		[PMID: 22853995]
    HEK293 IC50
    6 1
    Compound: MK-0431
    Inhibition of human DPP4 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
    Inhibition of human DPP4 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
    		[PMID: 22853995]
    HEK293 IC50
    11 3
    Compound: MK-0431
    Inhibition of human DPP8 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
    Inhibition of human DPP8 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
    		[PMID: 22853995]
    HEK293 IC50
    11 3
    Compound: MK-0431
    Inhibition of human DPP8 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
    Inhibition of human DPP8 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
    		[PMID: 22853995]
    HEK293 IC50
    20 3
    Compound: MK-0431
    Inhibition of human DPP9 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
    Inhibition of human DPP9 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
    		[PMID: 22853995]
    HEK293 IC50
    20 3
    Compound: MK-0431
    Inhibition of human DPP9 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
    Inhibition of human DPP9 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
    		[PMID: 22853995]
    HEK293 IC50
    22 1
    Compound: Sitagliptin Phosphate
    Inhibition of recombinant human DPP-4 expressed in HEK293 cells using H-Gly-Pro-AMC as substrate measured over 15 mins by fluorescence analysis
    Inhibition of recombinant human DPP-4 expressed in HEK293 cells using H-Gly-Pro-AMC as substrate measured over 15 mins by fluorescence analysis
    		[PMID: 28128944]
    HEK293 IC50
    22 1
    Compound: Sitagliptin Phosphate
    Inhibition of recombinant human DPP-4 expressed in HEK293 cells using H-Gly-Pro-AMC as substrate measured over 15 mins by fluorescence analysis
    Inhibition of recombinant human DPP-4 expressed in HEK293 cells using H-Gly-Pro-AMC as substrate measured over 15 mins by fluorescence analysis
    		[PMID: 28128944]
    HEK293 IC50
    20 3
    Compound: MK-0431
    Inhibition of human DPP9 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
    Inhibition of human DPP9 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
    		[PMID: 22853995]
    HEK293 IC50
    6 1
    Compound: MK-0431
    Inhibition of human DPP4 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
    Inhibition of human DPP4 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
    		[PMID: 22853995]
    HEK293 IC50
    22 1
    Compound: Sitagliptin Phosphate
    Inhibition of recombinant human DPP-4 expressed in HEK293 cells using H-Gly-Pro-AMC as substrate measured over 15 mins by fluorescence analysis
    Inhibition of recombinant human DPP-4 expressed in HEK293 cells using H-Gly-Pro-AMC as substrate measured over 15 mins by fluorescence analysis
    		[PMID: 28128944]
    HEK293 IC50
    6 1
    Compound: MK-0431
    Inhibition of human DPP4 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
    Inhibition of human DPP4 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
    		[PMID: 22853995]
    体外実験

    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 関連抗体
    体内実験

    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.
    臨床実験
    分子量

    505.31

    分子式

    C16H18F6N5O5P
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    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
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, sealed storage, away from moisture and light

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
    溶剤 & 溶解度
    体外: 

    DMSO : 100 mg/mL (197.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 50 mg/mL (98.95 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9790 mL 9.8949 mL 19.7898 mL
    5 mM 0.3958 mL 1.9790 mL 3.9580 mL
    10 mM 0.1979 mL 0.9895 mL 1.9790 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 and light). 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)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

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    体積 （開始）

    V1

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.95 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (4.95 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    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 (98.95 mM); Clear solution; Need ultrasonic

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

    Dosage

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    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).
    純度とドキュメンテーション

    純度: 99.88%

    COA (247 KB) HNMR (286 KB) RP-HPLC (222 KB) NP-HPLC (169 KB) MS (69 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    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 and light). 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 / DMSO 1 mM 1.9790 mL 9.8949 mL 19.7898 mL 49.4746 mL
    5 mM 0.3958 mL 1.9790 mL 3.9580 mL 9.8949 mL
    10 mM 0.1979 mL 0.9895 mL 1.9790 mL 4.9475 mL
    15 mM 0.1319 mL 0.6597 mL 1.3193 mL 3.2983 mL
    20 mM 0.0989 mL 0.4947 mL 0.9895 mL 2.4737 mL
    25 mM 0.0792 mL 0.3958 mL 0.7916 mL 1.9790 mL
    30 mM 0.0660 mL 0.3298 mL 0.6597 mL 1.6492 mL
    40 mM 0.0495 mL 0.2474 mL 0.4947 mL 1.2369 mL
    50 mM 0.0396 mL 0.1979 mL 0.3958 mL 0.9895 mL
    60 mM 0.0330 mL 0.1649 mL 0.3298 mL 0.8246 mL
    80 mM 0.0247 mL 0.1237 mL 0.2474 mL 0.6184 mL
    DMSO 100 mM 0.0198 mL 0.0989 mL 0.1979 mL 0.4947 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 Related Classifications

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    一般には略語で表示されます：C1V1 = C2V2

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    Keywords:

    Sitagliptin654671-78-0MK-0431MK0431MK 0431Dipeptidyl PeptidaseGLP ReceptorEndogenous MetabolitePKAERKDPPProtein kinase AExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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