1. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  2. PPAR
  3. Bezafibrate

Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.

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

CAS No. : 41859-67-0

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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of Bezafibrate:

Top Publications Citing Use of Products

    Bezafibrate purchased from MedChemExpress. Usage Cited in: Nat Genet. 2025 Mar;57(3):680-693.

    Western blot analysis of CPT1A and PD-L1 levels in cells treated with varying doses of Bezafibrate (BEZ).

    Bezafibrate purchased from MedChemExpress. Usage Cited in: Nat Genet. 2025 Mar;57(3):680-693.

    Tumor growth of B16F10 cells in immune-normal mice was assessed by treatment with control group, BEZ (Bezafibrate: 15 mg/kg) group, anti-CTLA-4 group, or a combination of both.

    Bezafibrate purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Apr 17:e2500272.  [Abstract]

    GFP‐specific fluorescence micrographs of HEK‐293T cells co‐transfected with (PGal4‐RXR,PPPARγ‐p65, P8UAS‐CMV) for 48 h in the presence or absence of 100 µM Bezafibrate.

    Bezafibrate purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Apr 17:e2500272.  [Abstract]

    C57BL/6J mice were s.c. injected with HEK 293 cells encapsulated in sodium alginate into the right flank on day 0, followed by s.c immunized on day 7, 14 for three total vaccinations. Bezafibrate (10mg /kg) was administrated i.p. every three days. Anti‐tumor effects of bezafibrate‐triggered target gene expression were assessed.

    Bezafibrate purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2023 Dec 25;8(1):457.  [Abstract]

    U87 cells with high EGFRvIII density were cocultured with EGFRvIII-targeted CAR-T cells, supplemented with indicated drugs. Cells were magnetically separated for CAR molecule detection. Representative immunoblotting images from three independent duplications showed that Atorvastatin (5μM, 3 days) and Cytochalasin (10μg/mL, 1 day) alleviated CAR molecule transfer.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.

    IC50 & Target[1]

    hPPARδ

    20 μM (EC50)

    hPPARα

    50 μM (EC50)

    hPPARγ

    60 μM (EC50)

    Cellular Effect
    Cell Line Type Value Description References
    CHO-K1 EC50
    > 137 μM
    Compound: Bezafibrate
    Concentration of compound that affords half-maximum transactivation of human Peroxisome proliferator activated receptor gamma in CHO-K1 cells was determined in vitro
    Concentration of compound that affords half-maximum transactivation of human Peroxisome proliferator activated receptor gamma in CHO-K1 cells was determined in vitro
    [PMID: 11738577]
    CHO-K1 EC50
    > 143 μM
    Compound: bezafibrate
    Agonist activity on Gal4 chimeric human Peroxisome proliferator activated receptor delta expressed in CHO-K1 cells
    Agonist activity on Gal4 chimeric human Peroxisome proliferator activated receptor delta expressed in CHO-K1 cells
    [PMID: 12904063]
    CHO-K1 EC50
    > 78 μM
    Compound: Bezafibrate
    Transactivation of human Peroxisome proliferator activated receptor alpha expressed in CHO-K1 cells
    Transactivation of human Peroxisome proliferator activated receptor alpha expressed in CHO-K1 cells
    [PMID: 11738577]
    COS-7 EC50
    15.4 μM
    Compound: Bezafibrate
    Agonist activity at Gal4-tagged human PPARgamma ligand binding domain expressed in COS-7 cells measured after overnight incubation by dual-glo luciferase reporter gene assay
    Agonist activity at Gal4-tagged human PPARgamma ligand binding domain expressed in COS-7 cells measured after overnight incubation by dual-glo luciferase reporter gene assay
    10.1039/C6MD00042H
    COS-7 EC50
    22.6 μM
    Compound: Bezafibrate
    Agonist activity at Gal4-tagged human PPARdelta ligand binding domain expressed in COS-7 cells measured after overnight incubation by dual-glo luciferase reporter gene assay
    Agonist activity at Gal4-tagged human PPARdelta ligand binding domain expressed in COS-7 cells measured after overnight incubation by dual-glo luciferase reporter gene assay
    10.1039/C6MD00042H
    COS-7 EC50
    7.1 μM
    Compound: Bezafibrate
    Agonist activity at Gal4-tagged human PPARalpha ligand binding domain expressed in COS-7 cells measured after overnight incubation by dual-glo luciferase reporter gene assay
    Agonist activity at Gal4-tagged human PPARalpha ligand binding domain expressed in COS-7 cells measured after overnight incubation by dual-glo luciferase reporter gene assay
    10.1039/C6MD00042H
    CV-1 EC50
    100 μM
    Compound: 2, benzafibrate
    Agonist activity at human PPARgamma expressed in monkey CV1 cells by transactivation assay
    Agonist activity at human PPARgamma expressed in monkey CV1 cells by transactivation assay
    [PMID: 18280733]
    CV-1 EC50
    110 μM
    Compound: 3
    Compound was tested for its agonist activity against murine Peroxisome proliferator activated receptor delta-GAL4 chimeric receptor in transfected CV-1 cells
    Compound was tested for its agonist activity against murine Peroxisome proliferator activated receptor delta-GAL4 chimeric receptor in transfected CV-1 cells
    [PMID: 10508427]
    CV-1 EC50
    20 μM
    Compound: 3
    Compound was tested for agonist activity on human Peroxisome proliferator activated receptor delta-GAL4 chimeric receptor in transfected CV-1 cells
    Compound was tested for agonist activity on human Peroxisome proliferator activated receptor delta-GAL4 chimeric receptor in transfected CV-1 cells
    [PMID: 10508427]
    CV-1 EC50
    3 μM
    Compound: benzafibrate
    Agonist activity at human PPARgamma expressed in CV1 cells by transactivation assay
    Agonist activity at human PPARgamma expressed in CV1 cells by transactivation assay
    [PMID: 17964792]
    CV-1 EC50
    30 μM
    Compound: 2, benzafibrate
    Agonist activity at human PPARalpha expressed in monkey CV1 cells by transactivation assay
    Agonist activity at human PPARalpha expressed in monkey CV1 cells by transactivation assay
    [PMID: 18280733]
    CV-1 EC50
    30 μM
    Compound: 2, benzafibrate
    Agonist activity at human PPARdelta expressed in monkey CV1 cells by transactivation assay
    Agonist activity at human PPARdelta expressed in monkey CV1 cells by transactivation assay
    [PMID: 18280733]
    CV-1 EC50
    30 μM
    Compound: benzafibrate
    Agonist activity at human PPARalpha expressed in CV1 cells by transactivation assay
    Agonist activity at human PPARalpha expressed in CV1 cells by transactivation assay
    [PMID: 17964792]
    CV-1 EC50
    30 μM
    Compound: benzafibrate
    Agonist activity at human PPARdelta expressed in CV1 cells by transactivation assay
    Agonist activity at human PPARdelta expressed in CV1 cells by transactivation assay
    [PMID: 17964792]
    CV-1 EC50
    50 μM
    Compound: 3
    Compound was tested for agonist activity on human Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor in transfected CV-1 cells
    Compound was tested for agonist activity on human Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor in transfected CV-1 cells
    [PMID: 10508427]
    CV-1 EC50
    55 μM
    Compound: 3
    Compound was tested for its agonist activity against murine Peroxisome proliferator activated receptor gamma-Gal4 chimeric receptor in transfected CV-1 cells
    Compound was tested for its agonist activity against murine Peroxisome proliferator activated receptor gamma-Gal4 chimeric receptor in transfected CV-1 cells
    [PMID: 10508427]
    CV-1 EC50
    60 μM
    Compound: 3
    Compound was tested for agonist activity on human Peroxisome proliferator activated receptor gamma-Gal4 chimeric receptor in transfected CV-1 cells
    Compound was tested for agonist activity on human Peroxisome proliferator activated receptor gamma-Gal4 chimeric receptor in transfected CV-1 cells
    [PMID: 10508427]
    CV-1 EC50
    90 μM
    Compound: 3
    Compound was tested for its agonist activity against murine Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor transfected CV-1 cells
    Compound was tested for its agonist activity against murine Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor transfected CV-1 cells
    [PMID: 10508427]
    HEK293 EC50
    35.74 μM
    Compound: 1
    Agonist activity at human PPARdelta expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay
    Agonist activity at human PPARdelta expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay
    [PMID: 23265844]
    HEK293 EC50
    46.58 μM
    Compound: 1
    Agonist activity at human PPARalpha expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay
    Agonist activity at human PPARalpha expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay
    [PMID: 23265844]
    HEK293 EC50
    70.36 μM
    Compound: 1
    Agonist activity at human PPARgamma expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay
    Agonist activity at human PPARgamma expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay
    [PMID: 23265844]
    HepG2 EC50
    1.04 μM
    Compound: BZF
    Transactivation of PPAR transfected in human HepG2 cells after 20 hrs by luciferase reporter gene assay
    Transactivation of PPAR transfected in human HepG2 cells after 20 hrs by luciferase reporter gene assay
    [PMID: 23031596]
    HepG2 EC50
    1.05 μM
    Compound: Benzafibrate
    Transactivation of PPAR expressed in HepG2 cells after 20 hrs by luminescence assay
    Transactivation of PPAR expressed in HepG2 cells after 20 hrs by luminescence assay
    [PMID: 22381047]
    HepG2 EC50
    18.9 μM
    Compound: 1
    Agonist activity at human PPARdelta expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay
    Agonist activity at human PPARdelta expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay
    [PMID: 21215640]
    HepG2 EC50
    42.5 μM
    Compound: 1
    Agonist activity at human PPARalpha expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay
    Agonist activity at human PPARalpha expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay
    [PMID: 21215640]
    HepG2 EC50
    57.2 μM
    Compound: 1
    Agonist activity at human PPARgamma expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay
    Agonist activity at human PPARgamma expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay
    [PMID: 21215640]
    INS1(832/13) EC50
    6 nM
    Compound: 36
    Induction of glucose-stimulated insulin secretion in rat INS-1 832/13 cells incubated for 5 mins by ELISA assay
    Induction of glucose-stimulated insulin secretion in rat INS-1 832/13 cells incubated for 5 mins by ELISA assay
    [PMID: 33771587]
    Sf21 IC50
    231.7 μM
    Compound: Bezafibrate
    Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    [PMID: 21965623]
    Sf21 IC50
    391 μM
    Compound: Bezafibrate
    Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    [PMID: 21965623]
    In Vitro

    Bezafibrate is an agonist of PPAR, with EC50s of 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, and 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, respectively[1].
    Bezafibrate (> 200 μM) shows significant cytotoxicity against human retinal microvascular endothelial cells (HRMECs) and human retinal pigment epithelial ARPE-19 cells. Bezafibrate (30-100 μM) suppresses tumor necrosis factor (TNF)α induced inflammatory factors and regulates TNFα induced nuclear factor (NF)-κB transactivation in HRMEC. Bezafibrate inhibits VEGF-induced HRMECs migration, and inhibits interleukin (IL)-1β-induced VEGF secretion of ARPE-19 cells[2].

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

    In Vivo

    Bezafibrate (0.5%) markedly reduces plasma lipid and glucose levels, and increases islet area in the pancreas in TallyHo mice. Bezafibrate also improves energy expenditure and metabolic flexibility. Moreover, Bezafibrate ameliorates steatosis, modifies lipid composition and increases mitochondrial mass in the liver[3].

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

    Clinical Trial
    Molecular Weight

    361.82

    Formula

    C19H20ClNO4

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC(C)(OC1=CC=C(CCNC(C2=CC=C(Cl)C=C2)=O)C=C1)C(O)=O

    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 (138.19 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7638 mL 13.8190 mL 27.6381 mL
    5 mM 0.5528 mL 2.7638 mL 5.5276 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 (6.91 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (6.91 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    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

    Purity: 99.83%

    References
    Cell Assay
    [2]

    Cell viability is assessed using the CCK-8 kit. Hhuman retinal microvascular endothelial cells (HRMECs) or ARPE-19 cells are seeded at 5000 cells/well in medium containing 10% serum in 96-well plates. After a 24-h incubation, the medium is serum-starved with 1% FBS for 6 h, the CCK-8 reagent is added, and the absorbance of the resultant solution is measured at 450 nm by using a microplate reader at three time points, 24, 48, and 72 h after treatment with Bezafibrate (0, 10, 50, 100, 200, 500, and 1000 μM)[2].

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

    Animal Administration
    [3]

    TallyHo mice are bred in our animal facility. Only male mice are used in the study, and mice receive a standard diet (SD), which is supplemented with 0.5% (w/w) Bezafibrate for the Bezafibrate groups for 8 weeks. Animals are killed by isoflurane overdose, and dissected tissues are prepared as stated below. All data represent samples taken after 8 weeks of Bezafibrate (or SD) treatment unless otherwise stated[3].

    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 2.7638 mL 13.8190 mL 27.6381 mL 69.0951 mL
    5 mM 0.5528 mL 2.7638 mL 5.5276 mL 13.8190 mL
    10 mM 0.2764 mL 1.3819 mL 2.7638 mL 6.9095 mL
    15 mM 0.1843 mL 0.9213 mL 1.8425 mL 4.6063 mL
    20 mM 0.1382 mL 0.6910 mL 1.3819 mL 3.4548 mL
    25 mM 0.1106 mL 0.5528 mL 1.1055 mL 2.7638 mL
    30 mM 0.0921 mL 0.4606 mL 0.9213 mL 2.3032 mL
    40 mM 0.0691 mL 0.3455 mL 0.6910 mL 1.7274 mL
    50 mM 0.0553 mL 0.2764 mL 0.5528 mL 1.3819 mL
    60 mM 0.0461 mL 0.2303 mL 0.4606 mL 1.1516 mL
    80 mM 0.0345 mL 0.1727 mL 0.3455 mL 0.8637 mL
    100 mM 0.0276 mL 0.1382 mL 0.2764 mL 0.6910 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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