1. Membrane Transporter/Ion Channel Metabolic Enzyme/Protease
  2. SGLT Endogenous Metabolite GLUT
  3. Phloretin

Phloretin  (Synonyms: NSC 407292; RJC 02792)

Cat. No.: HY-N0142 Purity: 99.92%
Handling Instructions Technical Support

Phloretin (NSC 407292; RJC 02792) is a flavonoid extracted from Malus pumila Mill.,has anti-inflammatory activities. Phloridzin is a specific,competitive and orally active inhibitor of sodium/glucose cotransporters in the intestine (SGLT1) and kidney (SGLT2). Phloretin inhibits Yeast-made GLUT1 as well as Human erythrocyte GLUT1 with IC50values of 49 μM and 61 μM,respectively.Phloretin has the potential for the treatment of rheumatoid arthritis (RA) and allergic airway inflammation.

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

CAS No. : 60-82-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 24 publication(s) in Google Scholar

Other Forms of Phloretin:

Top Publications Citing Use of Products

    Phloretin purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2022 Nov;54(11):2007-2021.  [Abstract]

    Huh7 cells were treated with sorafenib (5 μM) and/or Phloretin (50 and 100 μM) for 24 h.

    Phloretin purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2022 Nov;54(11):2007-2021.  [Abstract]

    Huh7 cells were pretreated with1μMinsulin to activate glucose transport, and then treated with Canagliflozin (20 μM) or Phloretin(100 μM) for 1 hour before measurement of glucose uptake.

    Phloretin purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2021 Jan;11(1):143-155.  [Abstract]

    Effect of Phloretin (50 μM) or lonidamine (50 μM) on DM-αKG-induced pyroptosis. HeLa cells were pretreated with phloretin or lonidamine for 2 hours.

    Phloretin purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2021 Jan;11(1):143-155.  [Abstract]

    Effect of Phloretin (50 μM) or lonidamine (50 μM) on DM-αKG induced intracellular pH. HeLa cells were pretreated with phloretin or lonidamine for 2 hours.

    Phloretin purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2021 Jan;11(1):143-155.  [Abstract]

    Effect of Phloretin (50 μM) or lonidamine (50 μM) on DM-αKG induced L-2HG levels. HeLa cells were pretreated with phloretin or lonidamine for 2 hours.

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    • Biological Activity

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    Description

    Phloretin (NSC 407292; RJC 02792) is a flavonoid extracted from Malus pumila Mill.,has anti-inflammatory activities. Phloridzin is a specific,competitive and orally active inhibitor of sodium/glucose cotransporters in the intestine (SGLT1) and kidney (SGLT2). Phloretin inhibits Yeast-made GLUT1 as well as Human erythrocyte GLUT1 with IC50values of 49 μM and 61 μM,respectively[1].Phloretin has the potential for the treatment of rheumatoid arthritis (RA) and allergic airway inflammation[4].

    IC50 & Target[1]

    SGLT1

     

    SGLT2

     

    Microbial Metabolite

     

    GLUT1

     

    GLUT2

     

    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    12.4 μM
    Compound: 9h
    Inhibition of human SGLT1 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay
    Inhibition of human SGLT1 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay
    [PMID: 28098449]
    HEK293 IC50
    18.3 μM
    Compound: 9h
    Inhibition of human SGLT2 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay
    Inhibition of human SGLT2 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay
    [PMID: 28098449]
    HEK293 IC50
    90 μM
    Compound: 4788
    Inhibition of the Sodium/Hydrogen Exchanger-Like Domain-Containing Protein 2 (NHA2, SLC9B2) as assessed by a sensor pH-sensitive genetically encoded fluorescent sensor (pHAxensor) in HEK-293 cells stably transfected with SLC9B2 (PubChem AID: 1794821)
    Inhibition of the Sodium/Hydrogen Exchanger-Like Domain-Containing Protein 2 (NHA2, SLC9B2) as assessed by a sensor pH-sensitive genetically encoded fluorescent sensor (pHAxensor) in HEK-293 cells stably transfected with SLC9B2 (PubChem AID: 1794821)
    10.5281/zenodo.7360521
    K562 IC50
    41 μM
    Compound: Phloretin
    Inhibition of NF-kappaB transactivation in TNF-alpha-stimulated human K562 cells preincubated for 2 hrs followed by TNF-alpha challenge measured after 6 hrs by dual luciferase reporter gene assay
    Inhibition of NF-kappaB transactivation in TNF-alpha-stimulated human K562 cells preincubated for 2 hrs followed by TNF-alpha challenge measured after 6 hrs by dual luciferase reporter gene assay
    [PMID: 24775915]
    MCF7 IC50
    7 μM
    Compound: Phloretin
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 6 days by SRB assay
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 6 days by SRB assay
    [PMID: 33257172]
    MCF7 IC50
    > 10 μM
    Compound: 5b
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 26690274]
    MDA-MB-231 IC50
    > 10 μM
    Compound: 5b
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 26690274]
    NCI-H1299 IC50
    54 μM
    Compound: Phloretin
    Cytotoxicity against human H1299 cells assessed as growth inhibition after 48 hrs by MTT assay
    Cytotoxicity against human H1299 cells assessed as growth inhibition after 48 hrs by MTT assay
    [PMID: 24200808]
    Oocyte IC50
    14 μM
    Compound: Phloretin
    TP_TRANSPORTER: inhibition of lactate uptake in Xenopus laevis oocytes
    TP_TRANSPORTER: inhibition of lactate uptake in Xenopus laevis oocytes
    [PMID: 10417314]
    Oocyte IC50
    28 μM
    Compound: Phloretin
    TP_TRANSPORTER: inhibition of lactate uptake in Xenopus laevis oocytes
    TP_TRANSPORTER: inhibition of lactate uptake in Xenopus laevis oocytes
    [PMID: 10417314]
    Oocyte IC50
    41 μM
    Compound: Phloretin
    TP_TRANSPORTER: inhibition of L-Lactate uptake (L-Lactate:30mM) in Xenopus laevis oocytes
    TP_TRANSPORTER: inhibition of L-Lactate uptake (L-Lactate:30mM) in Xenopus laevis oocytes
    [PMID: 11101640]
    Vero CC50
    735.47 μg/mL
    Compound: 31
    Cytotoxicity against african green monkey Vero cells assessed as cell death after 72 hrs by MTT assay
    Cytotoxicity against african green monkey Vero cells assessed as cell death after 72 hrs by MTT assay
    [PMID: 22169259]
    Vero IC50
    125 μg/mL
    Compound: 31
    Cytotoxicity against African green monkey Vero cells assessed as inhibition of cell growth after 72 hrs by MTT assay
    Cytotoxicity against African green monkey Vero cells assessed as inhibition of cell growth after 72 hrs by MTT assay
    [PMID: 22169259]
    In Vitro

    Phloretin induced obvious cytotoxicity against BEL-7402 cells with IC50 of 89.23 μM[2].
    Phloretin (40-160 μM; 24 hours) induces BEL-7402 cell apoptosis though the mitochondrial pathway,the cells exposed to phloretin exhibits nuclear chromatin condensation and increased fluorescence intensity. The caspase-9 reaches the peak level at 12 h,and leak levels of caspase-6 and caspase-3 activities occurrs 18 and 24 h after the exposure,respectively[2].
    Phloretin (0-100 μM; 24 hours) has effects on transcription factors of adipogenesis in differentiated 3T3-L1 adipocytes,decreases PPAR-γ,C/EBPα and C/EBPβ as a dose-dependent manner[3].
    Phloretin (0-100 μM; 24 hours) has effects on the AMPK pathway in differentiated 3T3-L1 adipocytes,increases the phosphorylation of substrate ACC-1,AMPK in PT-treated cells[3].

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

    Apoptosis Analysis[2]

    Cell Line: BEL-7402 cell
    Concentration: 40-160 μM
    Incubation Time: 24 hours
    Result: Induced cell apoptosis and activated caspase 3, 6 and 9.

    Western Blot Analysis[3]

    Cell Line: 3T3-L1 adipocytes
    Concentration: 0 μM, 3 μM, 10 μM, 30 μM, 100 μM
    Incubation Time: 24 hours
    Result: Inhibited PPAR-γ, C/EBPα and C/EBPβ expression.

    Western Blot Analysis[3]

    Cell Line: 3T3-L1 adipocytes
    Concentration: 0 μM, 3 μM, 10 μM, 30 μM, 100 μM
    Incubation Time: 24 hours
    Result: Upregulated the expression of p-ACC-1, p-AMPK, p-AMPKα and β .
    In Vivo

    Phloretin (oral administration; 50 or 100 mg/kg; once daily) decreases oxidative stress and diminished levels of malondialdehyde (MDA) and hydrogen peroxide in paw tissue,reduces productivity of anti-collagen antibodies in serum[3].

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

    Animal Model: Collagen-Induced Arthritis (CIA) Mice[3]
    Dosage: 50 or 100 mg/kg
    Administration: Oral adminstration
    Result: Showed mitigation of clinical symptoms of RA in addition to reduced inflammation of hind-limbs compared to the control group.
    Molecular Weight

    274.27

    Formula

    C15H14O5

    CAS No.
    Appearance

    Solid

    Color

    Off-white to pink

    SMILES

    O=C(C1=C(O)C=C(O)C=C1O)CCC2=CC=C(O)C=C2

    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 : 50 mg/mL (182.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.6460 mL 18.2302 mL 36.4604 mL
    5 mM 0.7292 mL 3.6460 mL 7.2921 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
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    Concentration (final)

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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 (9.12 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 (9.12 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Dosing volume
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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
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    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

    Purity: 99.92%

    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 3.6460 mL 18.2302 mL 36.4604 mL 91.1511 mL
    5 mM 0.7292 mL 3.6460 mL 7.2921 mL 18.2302 mL
    10 mM 0.3646 mL 1.8230 mL 3.6460 mL 9.1151 mL
    15 mM 0.2431 mL 1.2153 mL 2.4307 mL 6.0767 mL
    20 mM 0.1823 mL 0.9115 mL 1.8230 mL 4.5576 mL
    25 mM 0.1458 mL 0.7292 mL 1.4584 mL 3.6460 mL
    30 mM 0.1215 mL 0.6077 mL 1.2153 mL 3.0384 mL
    40 mM 0.0912 mL 0.4558 mL 0.9115 mL 2.2788 mL
    50 mM 0.0729 mL 0.3646 mL 0.7292 mL 1.8230 mL
    60 mM 0.0608 mL 0.3038 mL 0.6077 mL 1.5192 mL
    80 mM 0.0456 mL 0.2279 mL 0.4558 mL 1.1394 mL
    100 mM 0.0365 mL 0.1823 mL 0.3646 mL 0.9115 mL
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