Benzbromarone

Catalog No.S4221

Benzbromarone Chemical Structure

Molecular Weight(MW): 424.08

Benzbromarone is a CYP2C9 inhibitor, it binds to CYP2C9 with Ki value of 19.3 nM.

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Biological Activity

Description Benzbromarone is a CYP2C9 inhibitor, it binds to CYP2C9 with Ki value of 19.3 nM.
Targets
CYP2C9 [1]
19.3 nM(Ki)
In vitro

Benzbromarone (20 μM) decreases mitochondrial membrane potential by 81% in isolated rat hepatocytes. Benzbromarone decreases state 3 oxidation and respiratory control ratios for L-glutamate with IC50 < 1 μM in isolated rat liver mitochondria. Benzbromarone (50 μM) uncouples oxidative phosphorylation and increases oxygen consumption by hepatocytes starting at 10 μM in isolated rat hepatocytes. Benzbromarone also inhibits the formation of acid-soluble β-oxidation products in a dose-dependent manner with IC50 of 2 μM. Benzbromarone (100 μM) inhibits the electron transport chain and are uncouplers of oxidative phosphorylation in isolated rat liver mitochondria. Benzbromarone (1 μM) leads to concentration-dependent increasion of ROS production in HepG2 cells. Benzbromarone (100 μM) leads to a significant increase in mitochondrial size of isolated rat liver mitochondria. Benzbromarone is associated with leakage of cytochrome c into the cytoplasm of HepG2 cells. Benzbromarone (100 μM) results in the proportion of apoptotic cells of 11% in rat hepatocytes. [2] Benzbromarone significantly reduces the oxypurinol uptake at a concentration as low as 10 nM and completely blocks it at 1 μM. Benzbromarone (1 μM) uptakes the typical substrate of OCTN1 (tetraethylammonium) and OCTN2 (carnitine) in the HEK293 cells expressed with human OCTN1 by 96.7% and 111% of control, respectively. [3] Benzbromarone completely inhibits urate uptake at 50 μM in URAT1-expressing oocytes, with IC50 of less than 0.1 μM. [4] Benzbromarone activates through sequential hydroxylation of the benzofuran ring to a catechol, which can then be further oxidized to a reactive quinone intermediate capable of adducting protein. [5]

Protocol

Solubility (25°C)

In vitro DMSO 85 mg/mL (200.43 mM)
Ethanol 9 mg/mL (21.22 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 424.08
Formula

C17H12Br2O3

CAS No. 3562-84-3
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03534037 Active not recruiting Hyperuricemia|Metabolic Syndrome|Left Ventricular Diastolic Dysfunction National Defense Medical Center Taiwan December 3 2018 Phase 4
NCT03534037 Active not recruiting Hyperuricemia|Metabolic Syndrome|Left Ventricular Diastolic Dysfunction National Defense Medical Center Taiwan December 3 2018 Phase 4
NCT03185793 Recruiting Hyperuricemia Jiangsu HengRui Medicine Co. Ltd. May 11 2017 Phase 2
NCT03185793 Recruiting Hyperuricemia Jiangsu HengRui Medicine Co. Ltd. May 11 2017 Phase 2
NCT03100318 Completed Hyperuricemia With or Without Gout Fuji Yakuhin Co. Ltd.|Mochida Pharmaceutical Company Ltd. April 1 2017 Phase 3
NCT03100318 Completed Hyperuricemia With or Without Gout Fuji Yakuhin Co. Ltd.|Mochida Pharmaceutical Company Ltd. April 1 2017 Phase 3

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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P450 (e.g. CYP17) Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID