2. Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation NF-κB MAPK/ERK Pathway Cell Cycle/DNA Damage
  3. Xanthine Oxidase Apoptosis Interleukin Related Keap1-Nrf2 SOD Caspase Bcl-2 Family NF-κB JNK HSP
  4. Benzbromarone

Benzbromarone is an orally active anti-gout agent. Benzbromarone has anti-infammatory, anti-oxidative stress and nephroprotective effects. Benzbromarone can be used for the research of hyperuricemia and gout.

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

CAS No. : 3562-84-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
Solid
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Benzbromarone:

Benzbromarone Related Antibodies

Top Publications Citing Use of Products

    Benzbromarone purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Dec;15(12):6382-6398.

    Inhibition of 14C-urate transport by Benzbromarone in URAT1EM and its mutants.

    Benzbromarone purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Aug;10(24):e2300881.  [Abstract]

    Benzbromarone (BBR) (1-100 μM; 72 h) inhibited in vitro proliferation of multiple human GC and CRC cell lines.

    Benzbromarone purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Aug;10(24):e2300881.  [Abstract]

    Benzbromarone (BBR) (50 mg/kg; p.o.; once every other day for 3 weeks) showed anti-tumor effectiveness in ANO1-positive GC PDX mice.

    Benzbromarone purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Aug;10(24):e2300881.  [Abstract]

    Benzbromarone (BBR) (50 mg/kg; p.o.; once every other day for 3 weeks) evidently augmented the anti-tumor effect of anti-PD-1 antibody against MC38/CT26 xenograft mice.

    Benzbromarone purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Aug;10(24):e2300881.  [Abstract]

    Benzbromarone (BBR) (1-100 μM) dose-dependently inhibited ANO1's protein expression in multiple GI cancer cells.

    View All Interleukin Related Isoform Specific Products:

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    IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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    View All Isoforms
    Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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    Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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    NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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    JNK1 JNK2 JNK3 JNK

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    HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Benzbromarone is an orally active anti-gout agent. Benzbromarone has anti-infammatory, anti-oxidative stress and nephroprotective effects. Benzbromarone can be used for the research of hyperuricemia and gout[1][2][3][4].

    IC50 & Target

    IL-1β

     

    IL-8

     

    Caspase-8

     

    Caspase 9

     

    Caspase 3

     

    Bcl-2

     

    Cellular Effect
    Cell Line Type Value Description References
    HEK-293T IC50
    0.12 μM
    Compound: 2
    Inhibition of human URAT1 expressed in HEK293T cells assessed as reduction in [14C]uric acid uptake measured after 5 mins by liquid scintillation counting method
    Inhibition of human URAT1 expressed in HEK293T cells assessed as reduction in [14C]uric acid uptake measured after 5 mins by liquid scintillation counting method
    		[PMID: 28351592]
    HEK293 IC50
    0.3 μM
    Compound: benzbromarone
    Inhibition of human URAT1-mediated urate uptake in HEK293 cells
    Inhibition of human URAT1-mediated urate uptake in HEK293 cells
    		[PMID: 17325024]
    MDCK EC50
    39 μM
    Compound: 21
    Antiviral activity against Influenza A virus A/PR/8/34 (H1N1) infected in MDCK cells assessed as reduction in plaque formation after 2 days by plaque reduction assay
    Antiviral activity against Influenza A virus A/PR/8/34 (H1N1) infected in MDCK cells assessed as reduction in plaque formation after 2 days by plaque reduction assay
    		[PMID: 27046062]
    MDCK EC50
    39 μM
    Compound: 3
    Antiviral activity against Influenza A virus (A/PR/8/34) (H1N1) infected in MDCK cells assessed as reduction in plaque formation after 48 hrs by plaque reduction assay
    Antiviral activity against Influenza A virus (A/PR/8/34) (H1N1) infected in MDCK cells assessed as reduction in plaque formation after 48 hrs by plaque reduction assay
    		[PMID: 25856229]
    MDCK IC50
    35 nM
    Compound: 7, benzbromarone
    Inhibition of human URAT1 expressed in human MDCK cells
    Inhibition of human URAT1 expressed in human MDCK cells
    		[PMID: 21449597]
    Oocyte IC50
    22 μM
    Compound: Benzobromaron
    TP_TRANSPORTER: inhibition of lactate uptake in Xenopus laevis oocytes
    TP_TRANSPORTER: inhibition of lactate uptake in Xenopus laevis oocytes
    		[PMID: 10417314]
    Oocyte IC50
    9 μM
    Compound: Benzobromaron
    TP_TRANSPORTER: inhibition of lactate uptake in Xenopus laevis oocytes
    TP_TRANSPORTER: inhibition of lactate uptake in Xenopus laevis oocytes
    		[PMID: 10417314]
    RPTEC IC50
    6.8 μM
    Compound: BBR
    Inhibition of uric acid uptake in human RPTEC
    Inhibition of uric acid uptake in human RPTEC
    		[PMID: 33684442]
    S2 IC50
    4.6 μM
    Compound: Benzbromarone
    TP_TRANSPORTER: inhibition of Urate uptake (Urate: 300 uM) in OAT1-expressing S2 cells
    TP_TRANSPORTER: inhibition of Urate uptake (Urate: 300 uM) in OAT1-expressing S2 cells
    		[PMID: 12472777]
    Sf9 IC50
    4 μM
    Compound: Benzbromarone
    Inhibition of Homo sapiens (human) MRP1 expressed in Sf9 cell membranes assessed as decrease in N-ethyl-maleimide-glutathione-induced inorganic phosphate production by spectrophotometric analysis in presence of glutathione
    Inhibition of Homo sapiens (human) MRP1 expressed in Sf9 cell membranes assessed as decrease in N-ethyl-maleimide-glutathione-induced inorganic phosphate production by spectrophotometric analysis in presence of glutathione
    		10.1007/s00044-012-9994-0
    Sf9 IC50
    4 μM
    Compound: Benzbromarone
    Inhibition of human MRP1 expressed in Spodoptera frugiperda Sf9 cells assessed as inhibition of NEM-GS-induced vanadate-sensitive ATPase activity measured by generation of inorganic phosphate by spectrophotometry in presence of glutathione
    Inhibition of human MRP1 expressed in Spodoptera frugiperda Sf9 cells assessed as inhibition of NEM-GS-induced vanadate-sensitive ATPase activity measured by generation of inorganic phosphate by spectrophotometry in presence of glutathione
    		[PMID: 21530277]
    Vero IC50
    31.83 μg/mL
    Compound: Benzbromarone
    Cytotoxicity against african green monkey Vero cells measured after 48 hrs by MTT assay
    Cytotoxicity against african green monkey Vero cells measured after 48 hrs by MTT assay
    		[PMID: 38547733]
    In Vitro

    Benzbromarone (5-20 μM, 24 h) protects against propofol (HY-B0649)‑induced cytotoxicity in Human brain microvascular endothelial cells (HBMVECs)[1].
    Benzbromarone (5-20 μM, 24 h) mitigates propofol (HY-B0649)‑induced oxidative stress and inhibits expression of pro‑inflammatory cytokines and Chemokines in HBMVECs[1].
    Benzbromarone (1-100 μM, 2-24 h) activats the NRF2 signaling pathway in HepG2 cells[2].
    Benzbromarone (1-30 μM, 24 h) promotes degradation of HSP47 to ameliorate collagen overproduction in human keloid fibroblasts[3].

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

    Benzbromarone Related Antibodies

    Cell Cytotoxicity Assay[1]

    Cell Line: HBMVECs
    Concentration: 5 μM, 10 μM, 20 μM
    Incubation Time: 24 h
    Result: Improved the viability reduced by propofol.

    Western Blot Analysis[2]

    Cell Line: HepG2 cells
    Concentration: 1 μM, 2 μM, 5 μM, 10 μM, 20 μM, 50 μM, 100 μM
    Incubation Time: 2 h, 6 h, 24 h
    Result: Increased NRF2 protein expression in HepG2 cells exposed for 2 h, 6 h and 24 h at any concentration.
    Significantly accumulated the protein of NRF2 in the nuclear fraction after exposure to 100 μM at any time point.
    Caused an increase in the protein expression of TRX1 and TRX2.
    Significantly increased the ratio of oxidized TRX2 to reduced TRX2 at a concentration of 100 μM.
    In Vivo

    Benzbromarone (25-50 mg/kg, Intragastric, once a day for four weeks) aggravates hepatic steatosis in high fat diet (HFD)-induced obese (DIO) mice[3].
    Benzbromarone (10 mg/kg, Oral gavage, once a day for 14 consecutive days) attenuates the nephrotoxicity caused by cisplatin(HY-17394) in cisplatin treated rats[4].

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

    Animal Model: High fat diet (HFD)-induced obese (DIO) mice[3]
    Dosage: 25 mg/kg, 50 mg/kg
    Administration: Intragastric (i.g.)
    Result: Aggravated lipid accumulation in the liver of DIO mice.
    Significantly increased triglyceride accumulation and AST, ALT levels.
    Regulated multiple lipid metabolism genes and the expression of protein markers associated with apoptosis, endoplasmic reticulum stress, and inflammation in the liver of DIO mice.
    Animal Model: Cisplatin treated rats[2]
    Dosage: 10 mg/kg
    Administration: Oral gavage (p.o.)
    Result: Ameliorated the elevation in serum creatinine and blood urea nitrogen (BUN) levels induced by cisplatin.
    Counteracted oxidative stress induced by cisplatin and enhances anti-oxidant defenses in kidney.
    Alleviated the inflammatory events of nephrotoxicity induced by cisplatin.
    Attenuated cisplatin-induced apoptosis.
    Clinical Trial
    Molecular Weight

    424.08

    Formula

    C17H12Br2O3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=CC(Br)=C(O)C(Br)=C1)C2=C(CC)OC3=CC=CC=C23
    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 (235.80 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 2.3580 mL 11.7902 mL 23.5805 mL
    5 mM 0.4716 mL 2.3580 mL 4.7161 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)

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    Concentration
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    Volume
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    Molecular Weight *

    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)

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    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: ≥ 2.08 mg/mL (4.90 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 2.08 mg/mL (4.90 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:  15% Cremophor EL    85% Saline

      Solubility: 2.5 mg/mL (5.90 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

    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: 99.91%

    SDS (479 KB)

    COA (254 KB) HNMR (260 KB) RP-HPLC (250 KB) LCMS (98 KB)

    Handling Instructions (2659 KB)
    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 2.3580 mL 11.7902 mL 23.5805 mL 58.9511 mL
    5 mM 0.4716 mL 2.3580 mL 4.7161 mL 11.7902 mL
    10 mM 0.2358 mL 1.1790 mL 2.3580 mL 5.8951 mL
    15 mM 0.1572 mL 0.7860 mL 1.5720 mL 3.9301 mL
    20 mM 0.1179 mL 0.5895 mL 1.1790 mL 2.9476 mL
    25 mM 0.0943 mL 0.4716 mL 0.9432 mL 2.3580 mL
    30 mM 0.0786 mL 0.3930 mL 0.7860 mL 1.9650 mL
    40 mM 0.0590 mL 0.2948 mL 0.5895 mL 1.4738 mL
    50 mM 0.0472 mL 0.2358 mL 0.4716 mL 1.1790 mL
    60 mM 0.0393 mL 0.1965 mL 0.3930 mL 0.9825 mL
    80 mM 0.0295 mL 0.1474 mL 0.2948 mL 0.7369 mL
    100 mM 0.0236 mL 0.1179 mL 0.2358 mL 0.5895 mL
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    Benzbromarone Related Classifications

    Help & FAQs
    • 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:

    Benzbromarone3562-84-3Xanthine OxidaseApoptosisInterleukin RelatedKeap1-Nrf2SODCaspaseBcl-2 FamilyNF-κBJNKHSPXOILSuperoxide DismutaseNuclear factor-κBNuclear factor-kappaBc-Jun N-terminal kinaseHeat shock proteinsHuman brain microvascular endothelial cells (HBMVECs)HepG2 cellsHigh fat diet -induced obese micegoutInhibitorinhibitorinhibit

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