2. Membrane Transporter/Ion Channel Metabolic Enzyme/Protease Apoptosis
  3. URAT1 Oxidative Phosphorylation Apoptosis
  4. Benzarone

Benzarone  (Synonyms: Fragivix)

Cat. No.: HY-W011711 Purity: 99.67%
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Benzarone (Fragivix) is an oral inhibitor of human urate transporter 1 (hURAT1) with an IC50 value of 2.8 μM, and it also acts as an uncoupler of oxidative phosphorylation. Benzarone can cause liver damage and promote cell apoptosis and necrosis. Benzarone can be used to lower serum uric acid levels and for research in vascular diseases.

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

Benzarone Chemical Structure

Benzarone Chemical Structure

CAS No. : 1477-19-6

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Other Forms of Benzarone:

Benzarone Related Antibodies

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Description

Benzarone (Fragivix) is an oral inhibitor of human urate transporter 1 (hURAT1) with an IC50 value of 2.8 μM, and it also acts as an uncoupler of oxidative phosphorylation. Benzarone can cause liver damage and promote cell apoptosis and necrosis. Benzarone can be used to lower serum uric acid levels and for research in vascular diseases[1][2][3].

IC50 & Target

IC50: 2.8 μM (hURAT1 in oocyte)[1]
In Vitro

Benzarone (10-100 μM, 1 h) causes a reduction in mitochondrial membrane potential in isolated rat liver cells, decreases the oxidative status of L-glutamate and the respiration control ratio in rat liver mitochondria, and also leads to uncoupling of oxidative phosphorylation and a reduction in β-oxidation[2].
Benzarone (1 nM-100 μM, 1 h) increases the production of reactive oxygen species, causes leakage of cytochrome C from HepG2 cell mitochondria, and induces permeability transition in rat liver mitochondria along with apoptosis and necrosis in rat liver cells[2].

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

Benzarone Related Antibodies

Apoptosis Analysis[2]

Cell Line: HepG2
Concentration: 100 μM
Incubation Time: 8 h
Result: Caused fragmentation and condensation of chromatin, showing that 13% of the cells underwent apoptosis, along with cell death, and a decrease in ATP content.
In Vivo

Benzarone (0.5 mg/kg, taken orally, single dose) reaches a peak plasma concentration of 0.96 pg equivalent/mL in dogs one hour after administration. The area under the plasma concentration-time curve (AUC0-120h) is 43 pg equivalent h/mL, which is similar to the 3.8 pg equivalent•h/mL after intravenous administration, and binding reactions occur rapidly[3].
Benzarone (2 mg/kg, given by gavage, single dose) is excreted in bile in rats, undergoes metabolism through direct conjugation, and exhibits enterohepatic recirculation[3].

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

266.30

Formula

C17H14O3
CAS No.
Appearance

Solid

Color

Brown to gray

SMILES

O=C(C1=C(CC)OC2=CC=CC=C12)C3=CC=C(O)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (375.52 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 3.7552 mL 18.7758 mL 37.5516 mL
5 mM 0.7510 mL 3.7552 mL 7.5103 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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

×
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 (9.39 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.
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: 99.67%

COA (251 KB) HNMR (119 KB) RP-HPLC (217 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7552 mL 18.7758 mL 37.5516 mL 93.8791 mL
5 mM 0.7510 mL 3.7552 mL 7.5103 mL 18.7758 mL
10 mM 0.3755 mL 1.8776 mL 3.7552 mL 9.3879 mL
15 mM 0.2503 mL 1.2517 mL 2.5034 mL 6.2586 mL
20 mM 0.1878 mL 0.9388 mL 1.8776 mL 4.6940 mL
25 mM 0.1502 mL 0.7510 mL 1.5021 mL 3.7552 mL
30 mM 0.1252 mL 0.6259 mL 1.2517 mL 3.1293 mL
40 mM 0.0939 mL 0.4694 mL 0.9388 mL 2.3470 mL
50 mM 0.0751 mL 0.3755 mL 0.7510 mL 1.8776 mL
60 mM 0.0626 mL 0.3129 mL 0.6259 mL 1.5647 mL
80 mM 0.0469 mL 0.2347 mL 0.4694 mL 1.1735 mL
100 mM 0.0376 mL 0.1878 mL 0.3755 mL 0.9388 mL
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Benzarone 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:

Benzarone1477-19-6FragivixURAT1Oxidative PhosphorylationApoptosisUrate transporter 1SLC22A12hURAT1uric acidoxidative phosphorylationInhibitorinhibitorinhibit

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