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

Bromfenac sodium hydrate  (Synonyms: Bromfenac monosodium salt sesquihydrate)

Cat. No.: HY-B1888B Purity: 99.94%
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Bromfenac sodium hydrate (Bromfenac monosodium salt sesquihydrate) 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 hydrate can be used in ocular inflammation research.

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

Bromfenac sodium hydrate Chemical Structure

Bromfenac sodium hydrate Chemical Structure

CAS No. : 120638-55-3

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

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Description

Bromfenac sodium hydrate (Bromfenac monosodium salt sesquihydrate) 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 hydrate 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 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% (18h 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%; 50μL; 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%; 50μL; 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[3]
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%.
Animal Model: Male injected with Salin or BTX-B[4]
Dosage: 1 μL (0.09%) per eye
Administration: Eyedrop instillation; 1 μL (0.09%) per eye; twice-daily; 4 weeks
Result: Improved the corneal fluorescein staining score later at 4 weeks after treatment.
Clinical Trial
Molecular Weight

383.17

Formula

C15H14BrNNaO4.5

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.[1.5H2O]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (260.98 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 100 mg/mL (260.98 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6098 mL 13.0490 mL 26.0981 mL
5 mM 0.5220 mL 2.6098 mL 5.2196 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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: ≥ 2.5 mg/mL (6.52 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.52 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 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.

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:  PBS

    Solubility: 33.33 mg/mL (86.98 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.94%

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). 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 / H2O 1 mM 2.6098 mL 13.0490 mL 26.0981 mL 65.2452 mL
5 mM 0.5220 mL 2.6098 mL 5.2196 mL 13.0490 mL
10 mM 0.2610 mL 1.3049 mL 2.6098 mL 6.5245 mL
15 mM 0.1740 mL 0.8699 mL 1.7399 mL 4.3497 mL
20 mM 0.1305 mL 0.6525 mL 1.3049 mL 3.2623 mL
25 mM 0.1044 mL 0.5220 mL 1.0439 mL 2.6098 mL
30 mM 0.0870 mL 0.4350 mL 0.8699 mL 2.1748 mL
40 mM 0.0652 mL 0.3262 mL 0.6525 mL 1.6311 mL
50 mM 0.0522 mL 0.2610 mL 0.5220 mL 1.3049 mL
60 mM 0.0435 mL 0.2175 mL 0.4350 mL 1.0874 mL
80 mM 0.0326 mL 0.1631 mL 0.3262 mL 0.8156 mL
100 mM 0.0261 mL 0.1305 mL 0.2610 mL 0.6525 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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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