Cat. No.: HY-B1135

Benzbromarone

10 Cited Publications

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Based on 10 publication(s) in Google Scholar

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.

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Pureté: 99.91%
CAS No.: 3562-84-3
Formule: C₁₇H₁₂Br₂O₃
Masse moléculaire:424.08

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Benzbromarone Chemical Structure

CAS No.: 3562-84-3

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (10)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

IL-1β

IL-8

Caspase-8

Caspase 9

Caspase 3

Bcl-2

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Cellular Effect

Cell Line	Type	Value	Description	References
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]
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]
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]
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	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]
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 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]
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
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.

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 3562-84-3
Appearance Solid
Masse moléculaire 424.08
Formule C₁₇H₁₂Br₂O₃
Color White to off-white
SMILES

O=C(C1=CC(Br)=C(O)C(Br)=C1)C2=C(CC)OC3=CC=CC=C23
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (10)

All Cell Proliferation/Viability AssayBio/Physico-chemical AssayIn Vivo Efficacy StudyWB

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Journal Impact Factor

Nat Commun

Molecular mechanism of drug inhibition of URAT1. [Abstract]

2025 Jul 16;16(1):6551. PMID: 40670375
Acta Pharm Sin B

Generation and applications of an expandable and mature hiPSC-derived liver organoid. [Abstract]

2025 Dec;15(12):6382-6398. PMID: 41477334

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

Inhibition of ¹⁴C-urate transport by Benzbromarone in URAT1^EM and its mutants.
Adv Sci (Weinh)

Slow Metabolism-Driven Amplification of Hepatic PPARγ Agonism Mediates Benzbromarone-Induced Obesity-Specific Liver Injury. [Abstract]

2024 Nov 29:e2409126. PMID: 39611414
Adv Sci (Weinh)

ANO1-Mediated Inhibition of Cancer Ferroptosis Confers Immunotherapeutic Resistance through Recruiting Cancer-Associated Fibroblasts. [Abstract]

2023 Aug;10(24):e2300881. PMID: 37341301

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.
Phytother Res

α-Mangostin Attenuates Blood Pressure and Reverses Vascular Remodeling by Balancing ACE/AT1R and ACE2/Ang-(1-7)/MasR Axes in Ang II-Infused Hypertensive Mice. [Abstract]

2024 Dec;38(12):5918-5929. PMID: 39410864
Stem Cell Res Ther

Co-transplantation with adipose-derived cells to improve parathyroid transplantation in a mice model. [Abstract]

2020 May 26;11(1):200. PMID: 32456711
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576
Int Immunopharmacol

METTL14 downregulates GLUT9 through m6A methylation and attenuates hyperuricemia-induced fibrosis in mouse renal tubular epithelial cells. [Abstract]

2024 Oct 10;143(Pt 1):113308. PMID: 39393275
Biotechnol Bioeng

An integrated biomimetic array chip for establishment of collagen-based 3D primary human hepatocyte model for prediction of clinical drug-induced liver injury. [Abstract]

2021 Dec;118(12):4687-4698. PMID: 34478150
bioRxiv

2026 Apr 30.

Solvant et solubilité

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3580 mL

11.7902 mL

23.5805 mL

5 mM

0.4716 mL

2.3580 mL

4.7161 mL

10 mM

0.2358 mL

1.1790 mL

2.3580 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working 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: 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (288 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
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GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Huang Z, et al. The protective effects of benzbromarone against propofol-induced inflammation and injury in human brain microvascular endothelial cells (HBMVECs) [J]. Neurotoxicity Research, 2021, 39(5): 1449-1458. [Content Brief]

[2]. Roos N J, et al. The uricosuric benzbromarone disturbs the mitochondrial redox homeostasis and activates the NRF2 signaling pathway in HepG2 cells [J]. Free Radical Biology and Medicine, 2020, 152: 216-226. [Content Brief]

[3]. Park J G, et al. Benzbromarone Induces Targeted Degradation of HSP47 Protein and Improves Hypertrophic Scar Formation [J]. Journal of Investigative Dermatology, 2023. [Content Brief]

[4]. Sun P, et al. Benzbromarone aggravates hepatic steatosis in obese individuals [J]. Biochimica et Biophysica Acta (BBA)-Molecular Basis of Disease, 2018, 1864(6): 2067-2077. [Content Brief]

[5]. Abdel-Razek E A N, et al. Benzbromarone mitigates cisplatin nephrotoxicity involving enhanced peroxisome proliferator-activated receptor-alpha (PPAR-α) expression [J]. Life sciences, 2020, 243: 117272. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Benzbromarone

10 Cited Publications

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Benzbromarone

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Publications Citing Use of MedChemExpress (MCE) Benzbromarone

Voir tous les produits spécifiques à Isoform Interleukin Related

Voir tous les produits spécifiques à Isoform Caspase

Voir tous les produits spécifiques à Isoform Bcl-2 Family

Voir tous les produits spécifiques à Isoform NF-κB

Voir tous les produits spécifiques à Isoform JNK

Voir tous les produits spécifiques à Isoform HSP

Activité biologique

Chemical Information

Publications (10)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Benzbromarone Related Classifications

HY-B1135 Related Classifications