1. Immunology/Inflammation
  2. COX
  3. Bromfenac sodium

Bromfenac sodium is a potent and orally active inhibitor of COX, with IC50s of 5.56 and 7.45 nM for COX-1 and COX-2, respectively. Bromfenac sodium can be used in ocular inflammation research.

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

Bromfenac sodium Chemical Structure

Bromfenac sodium Chemical Structure

CAS No. : 91714-93-1

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Based on 1 publication(s) in Google Scholar

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Description

Bromfenac sodium is a potent and orally active inhibitor of COX, with IC50s of 5.56 and 7.45 nM for COX-1 and COX-2, respectively. Bromfenac sodium can be used in ocular inflammation research[1].

IC50 & Target[1]

COX-1

5.56 nM (IC50)

COX-2

7.45 nM (IC50)

In Vitro

Bromfenac (0-80 μg/mL; 24 h) can inhibit transforming growth factor-β2-induced epithelial-mesenchymal transition in HLEC-B3 in a concentration-dependent manner[2].
Bromfenac (80 μg/Ml; 48 h) inhibits transforming growth factor-β2-induced epithelial-mesenchymal transition in human anterior capsules[2].

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

Cell Viability Assay[2]

Cell Line: transforming growth factor-β2-treated human anterior capsules.
Concentration: 80 μg/mL
Incubation Time: 48 hours
Result: Suppressed transforming growth factor-β2-induced epithelial-mesenchymal transition in primary lens epithelial cells (LECs).

Cell Migration Assay [2]

Cell Line: HLEC-B3 cells
Concentration: 0, 20, 40, 60, and 80 μg/mL
Incubation Time: 24 hours
Result: Suppressed transforming growth factor-β2-induced cell migration in HLEC-B3 cells, and exhibited inhibition of the over-expression of epithelial-mesenchymal transition markers.
In Vivo

Bromfenac (0.0032-3.16%; 100 or 200 μL; rubbed onto the backs) produces significant anti-inflammatory activity at concentrations as low as 0.1% (4 h pretreatment time) or 0.32% (18 h pretreatment time) in rats[3].
Bromfenac (0.032-3.16%; 100 μL; rubbed onto the paws) produces dose-related anti-inflammatory activity in rats[3].
Bromfenac (0.032-1.0%; 50 μL) is 26 times more potent than indomethacin in blocking the erythema when applied directly onto the skin area exposed to UV light in guinea pigs[3].
Bromfenac (0.0032-0.1%; 50 μL; rubbed onto the uninjected paw for 4 h per day and 5 days per week) produces a dose and time dependent reduction in the paw volume of both hind limbs in rats[3].
Bromfenac (0.32%; 50 μL; rubbed onto the abdomen) produces significant blockade of abdominal constriction to ACh challenge in mice[3].
Bromfenac (eyedrop instillation; 1 μL (0.09%) per eye; twice-daily; 4 w) partially reduces corneal staining, and becomes so more slowly by the 4-week time point[4].

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

Animal Model: Male Sprague-Dawley rats (150-250 g) are injected carrageenan[2]
Dosage: 0.0032, 0.01, 0.032, 0.1, 0.32, 1.0, 3.16% (100 or 200 μL)
Administration: Rubbed onto the backs before 1-72 h of injected carrageenan
Result: Produced significant anti-inflammatory activity when applied 1, 2, and 4 h prior to carrageenan challenge at 0.32%.
Applied 1 or 4 h prior to carrageenan challenge was active, but not when applied 24 h (or longer) prior to challenge at 0.2%.
Clinical Trial
Molecular Weight

356.15

Formula

C15H11BrNNaO3

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(O[Na])CC1=CC=CC(C(C2=CC=C(Br)C=C2)=O)=C1N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 11.36 mg/mL (31.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8078 mL 14.0390 mL 28.0781 mL
5 mM 0.5616 mL 2.8078 mL 5.6156 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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: ≥ 1.14 mg/mL (3.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.14 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.4 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: ≥ 1.14 mg/mL (3.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.14 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.4 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.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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
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 (sealed storage, away from moisture and light). 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 2.8078 mL 14.0390 mL 28.0781 mL 70.1951 mL
5 mM 0.5616 mL 2.8078 mL 5.6156 mL 14.0390 mL
10 mM 0.2808 mL 1.4039 mL 2.8078 mL 7.0195 mL
15 mM 0.1872 mL 0.9359 mL 1.8719 mL 4.6797 mL
20 mM 0.1404 mL 0.7020 mL 1.4039 mL 3.5098 mL
25 mM 0.1123 mL 0.5616 mL 1.1231 mL 2.8078 mL
30 mM 0.0936 mL 0.4680 mL 0.9359 mL 2.3398 mL
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Bromfenac sodium 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.

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