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Benzbromarone P450 (e.g. CYP17) inhibitor

Name: Benzbromarone
Brand: Selleck Chemicals
SKU: S4221
Availability: InStock
Rating: 5 (3 reviews)

Catalog No.S4221 Purity:99.97%

Benzbromarone(Desuric) is a CYP2C9 inhibitor, it binds to CYP2C9 with K_i value of 19.3 nM.

Chemical Structure

Molecular Weight: 424.08

Purity & Quality Control

Batch: Purity: 99.97%

99.97

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Signaling Pathway

P450 (e.g. CYP17) Signaling Pathway

Mechanism of Action

Targets

CYP2C9 ^[1]

19.3 nM(Ki)

In vitro
In vitro	Benzbromarone (20 μM) decreases mitochondrial membrane potential by 81% in isolated rat hepatocytes. This compound decreases state 3 oxidation and respiratory control ratios for L-glutamate with IC50 < 1 μM in isolated rat liver mitochondria. It (50 μM) uncouples oxidative phosphorylation and increases oxygen consumption by hepatocytes starting at 10 μM in isolated rat hepatocytes. This chemical also inhibits the formation of acid-soluble β-oxidation products in a dose-dependent manner with IC50 of 2 μM. It (100 μM) inhibits the electron transport chain and are uncouplers of oxidative phosphorylation in isolated rat liver mitochondria. This compound (1 μM) leads to concentration-dependent increasion of ROS production in HepG2 cells. It (100 μM) leads to a significant increase in mitochondrial size of isolated rat liver mitochondria. This chemical is associated with leakage of cytochrome c into the cytoplasm of HepG2 cells. It (100 μM) results in the proportion of apoptotic cells of 11% in rat hepatocytes. ^[2] This compound significantly reduces the oxypurinol uptake at a concentration as low as 10 nM and completely blocks it at 1 μM. It (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] This chemical completely inhibits urate uptake at 50 μM in URAT1-expressing oocytes, with IC50 of less than 0.1 μM. ^[4] It 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]

References

https://pubmed.ncbi.nlm.nih.gov/12814975/
https://pubmed.ncbi.nlm.nih.gov/15799034/
https://pubmed.ncbi.nlm.nih.gov/16135657/

https://pubmed.ncbi.nlm.nih.gov/12024214/
https://pubmed.ncbi.nlm.nih.gov/18020424/

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Chemical Information

Molecular Weight	424.08	Formula	C₁₇H₁₂Br₂O₃
CAS No.	3562-84-3	SDF	Download SDF
Synonyms	Desuric
Smiles	CCC1=C(C2=CC=CC=C2O1)C(=O)C3=CC(=C(C(=C3)Br)O)Br

Storage and Stability

Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
			1 month-20°Cin solvent

In vitro
Batch:

DMSO : 85 mg/mL ( (200.43 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (23.58mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

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