1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. Diosmetin

Diosmetin is a natural flavonoid which inhibits human CYP1A enzyme activity with an IC50 of 40 μM in HepG2 cell.

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

CAS No. : 520-34-3

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Customer Review

Based on 20 publication(s) in Google Scholar

Other Forms of Diosmetin:

Top Publications Citing Use of Products

    Diosmetin purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2026 May:154:158036.  [Abstract]

    IC50 values ​​of ESCC cells after 48 h of Diosmetin (DIOS) treatment.

    Diosmetin purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2026 May:154:158036.  [Abstract]

    Effects of Diosmetin (DIOS) pretreated ESCC cell conditioned medium (CM) on migration, invasion, and tubular formation of human umbilical vein endothelial cells (HUVECs).

    Diosmetin purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2026 May:154:158036.  [Abstract]

    The expression levels of p-PI3K Tyr458, p-AKT Ser473, p-STAT4 Tyr693, and PDGFC, as well as the secretion level of PDGFC, were detected in ESCC cells after Diosmetin (DIOS) intervention.

    Diosmetin purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2026 May:154:158036.  [Abstract]

    Diosmetin (DIOS: 40 μM). Immunohistochemical staining image of CD31 in glue plug tissue.

    Diosmetin purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2026 May:154:158036.  [Abstract]

    SPR experiments showed that Diosmetin (DIOS: 40 μM) can bind directly to AURKB.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Diosmetin is a natural flavonoid which inhibits human CYP1A enzyme activity with an IC50 of 40 μM in HepG2 cell.

    IC50 & Target

    CYP1

     

    Cellular Effect
    Cell Line Type Value Description References
    HT-22 EC50
    59.7 μM
    Compound: 12
    Neuroprotective activity against glutamate-induced cell death in mouse HT-22 cells assessed as increase in cell viability after 24 hrs by EZ-Cytox assay
    Neuroprotective activity against glutamate-induced cell death in mouse HT-22 cells assessed as increase in cell viability after 24 hrs by EZ-Cytox assay
    [PMID: 32991171]
    HUVEC IC50
    7.6 μM
    Compound: 40, diosmetin
    Inhibition of NADPH oxidase in Homo sapiens (human) HUVEC cells
    Inhibition of NADPH oxidase in Homo sapiens (human) HUVEC cells
    10.1007/s00044-012-0353-y
    HepG2 EC50
    7.98 μM
    Compound: Diosmetin
    Antioxidant activity in human HepG2 cells assessed as decrease in fluorescence level after 2.5 hrs measured every 5 mins for 1 hr by DCFH-DA staining based fluorescence assay
    Antioxidant activity in human HepG2 cells assessed as decrease in fluorescence level after 2.5 hrs measured every 5 mins for 1 hr by DCFH-DA staining based fluorescence assay
    [PMID: 26974372]
    K562 IC50
    8.42 μM
    Compound: Diosmetin
    Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 24 to 48 hrs by MTS assay
    Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 24 to 48 hrs by MTS assay
    [PMID: 35551036]
    KBM5 IC50
    6.46 μM
    Compound: Diosmetin
    Antiproliferative activity against human KBM5 cells harbouring T315I mutant assessed as cell growth inhibition measured after 24 to 48 hrs by MTS assay
    Antiproliferative activity against human KBM5 cells harbouring T315I mutant assessed as cell growth inhibition measured after 24 to 48 hrs by MTS assay
    [PMID: 35551036]
    KBM5 IC50
    8.52 μM
    Compound: Diosmetin
    Antiproliferative activity against human KBM5 cells assessed as cell growth inhibition measured after 24 to 48 hrs by MTS assay
    Antiproliferative activity against human KBM5 cells assessed as cell growth inhibition measured after 24 to 48 hrs by MTS assay
    [PMID: 35551036]
    Monocyte IC50
    3 x 10-6 M
    Compound: diosmetin
    Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs
    Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs
    [PMID: 8882428]
    Neutrophil IC50
    0.7 μM
    Compound: 4g, Diosmetin
    Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of HOCl-induced oxidation of APF after 6 mins by fluorescence assay
    Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of HOCl-induced oxidation of APF after 6 mins by fluorescence assay
    [PMID: 23871908]
    Neutrophil IC50
    10.3 μM
    Compound: 4g, Diosmetin
    Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of H2O2-induced oxidation of amplex red incubated for 5 mins prior to PMA challenge by fluorescence assay
    Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of H2O2-induced oxidation of amplex red incubated for 5 mins prior to PMA challenge by fluorescence assay
    [PMID: 23871908]
    Neutrophil IC50
    15 μM
    Compound: 4g, Diosmetin
    Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of superoxide anion radical-induced lucigenin oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay
    Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of superoxide anion radical-induced lucigenin oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay
    [PMID: 23871908]
    Neutrophil IC50
    3.6 μM
    Compound: 4g, Diosmetin
    Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of ROS-induced luminol oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay
    Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of ROS-induced luminol oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay
    [PMID: 23871908]
    Peritoneal macrophage IC50
    8.9 μM
    Compound: 28; kp18
    Inhibition of LPS-stimulated nitric oxide production in ddy mouse peritoneal macrophages measured after 20 hrs by Greiss method
    Inhibition of LPS-stimulated nitric oxide production in ddy mouse peritoneal macrophages measured after 20 hrs by Greiss method
    [PMID: 27955927]
    RAW264.7 CC50
    > 100 μM
    Compound: 19
    Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
    Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
    [PMID: 33667099]
    RAW264.7 IC50
    16.7 μM
    Compound: 28; kp18
    Inhibition of LPS-stimulated nitric oxide production in mouse RAW264.7 cells by Greiss method
    Inhibition of LPS-stimulated nitric oxide production in mouse RAW264.7 cells by Greiss method
    [PMID: 27955927]
    RAW264.7 IC50
    32.2 μM
    Compound: 28; kp18
    Inhibition of LPS/INF-gamma-stimulated nitric oxide production in mouse RAW264.7 cells by Greiss method
    Inhibition of LPS/INF-gamma-stimulated nitric oxide production in mouse RAW264.7 cells by Greiss method
    [PMID: 27955927]
    RAW264.7 IC50
    34.5 μM
    Compound: 19
    Inhibition of LPS induced NO production in mouse RAW264.7 cells measured after 24 hrs by Griess reagent based assay
    Inhibition of LPS induced NO production in mouse RAW264.7 cells measured after 24 hrs by Griess reagent based assay
    [PMID: 33667099]
    RAW264.7 IC50
    8.4 μM
    Compound: 10
    Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as decrease in PGE2 production preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
    Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as decrease in PGE2 production preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
    [PMID: 31747281]
    In Vitro

    Diosmetin inhibits cell proliferation in HepG2 cells in a concentration-dependent manner. Untreated HepG2 cells grow well and are observed to have with normal skeletons, whereas cells treated with diosmetin are distorted and a number of them become round and floating[1].

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

    In Vivo

    Pretreatment with diosmetin significantly reduces serum levels of amylase and lipase; the histological injury; the secretion of tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and IL-6; myeloperoxidase (MPO) activity, trypsinogen activation peptide (TAP) level, the expression of inducible nitric oxide synthase (iNOS); and the nuclear factor (NF)-κB activation in cerulein-induced acute pancreatitis[2].

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

    Molecular Weight

    300.26

    Formula

    C16H12O6

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C1C=C(C2=CC=C(OC)C(O)=C2)OC3=CC(O)=CC(O)=C13

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (333.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.3304 mL 16.6521 mL 33.3041 mL
    5 mM 0.6661 mL 3.3304 mL 6.6608 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    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 (8.33 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.

    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:  0.5% CMC-Na/saline water

      Solubility: 10 mg/mL (33.30 mM); Suspended 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.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References
    Cell Assay
    [1]

    Diosmetin is dissolved in DMSO which is maintained at a constant concentration in control samples (2%). HepG2 cells are maintained in a humidified atmosphere of 5% CO2 at 37°C, and cultured in RPMI-1640 medium supplemented with 10% (v/v) fetal bovine serum, 100 U/mL penicillin and 100 U/mL streptomycin. HepG2 cell density is adjusted to 2×104 cells/100 μL, and the cells are seeded into 96-well plates and placed in an incubator overnight (37°C in 5% CO2) to allow for attachment and recovery. MTT analyses are performed. Briefly, cells are pretreated with 5, 10, 15 and 20 μg/mL diosmetin for 24 h. A total of 20 μL MTT solution (5 mg/mL in PBS) solution is transferred to each well to yield a final 120 μL/well and to separate wells a total of 10 μL CCK8 (5 mg/mL in PBS) is transferred. The plates are incubated for 4 h at 37°C in 5% CO2 and the absorbance is recorded at wavelengths of 595 nm and 450 nm, respectively. The half maximal inhibitory concentration (IC50) of diosmetin is calculated[1].

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

    Animal Administration
    [2]

    Experimental acute pancreatitis is induced in mice by seven intraperitoneal injection of cerulein (50 μg/kg) at hourly intervals. Diosmetin (100 mg/kg) or vehicle is pretreated 2 h before the first cerulein injection. After 6 h, 9 h, 12 h of the first cerulein injection, the severity of acute pancreatitis is evaluated biochemically and morphologically[2].

    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.3304 mL 16.6521 mL 33.3042 mL 83.2604 mL
    5 mM 0.6661 mL 3.3304 mL 6.6608 mL 16.6521 mL
    10 mM 0.3330 mL 1.6652 mL 3.3304 mL 8.3260 mL
    15 mM 0.2220 mL 1.1101 mL 2.2203 mL 5.5507 mL
    20 mM 0.1665 mL 0.8326 mL 1.6652 mL 4.1630 mL
    25 mM 0.1332 mL 0.6661 mL 1.3322 mL 3.3304 mL
    30 mM 0.1110 mL 0.5551 mL 1.1101 mL 2.7753 mL
    40 mM 0.0833 mL 0.4163 mL 0.8326 mL 2.0815 mL
    50 mM 0.0666 mL 0.3330 mL 0.6661 mL 1.6652 mL
    60 mM 0.0555 mL 0.2775 mL 0.5551 mL 1.3877 mL
    80 mM 0.0416 mL 0.2082 mL 0.4163 mL 1.0408 mL
    100 mM 0.0333 mL 0.1665 mL 0.3330 mL 0.8326 mL
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      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.

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