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

Bromfenac sodium 

Cat. No.: HY-B1888A Purity: 99.91%
Handling Instructions

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 is a brominated non-steroidal anti-inflammatory/analgesic drug (NSAID), and it is commonly used for the research of postoperative inflammation and pain following cataract surgery, and pseudophakic cystoid macular edema (CME).

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 is a brominated non-steroidal anti-inflammatory/analgesic drug (NSAID), and it is commonly used for the research of postoperative inflammation and pain following cataract surgery, and pseudophakic cystoid macular edema (CME)[1][2].

IC50 & Target[1]

COX-1

5.56 nM (IC50)

COX-2

7.45 nM (IC50)

In Vitro

Bromfenac (90 μg/mL; 48 h) inhibits TGF-b1-induced extracellular matrix (ECM) synthesis and myofibroblast activation in HConFs and HPFs[3].
Bromfenac (30-90 μg/mL; 48 h) decreases the protein and mRNA expression levels of FN, COL3, a-SMA, and survivin in a dose-dependent manner in HConFs and HPFs[3].
Bromfenac (30-90 μg/mL; 48 h) declines the phosphorylated protein levels of AKT, ERK1/2, and GSK-3b-S9 with dosage in HPFs and HConFs[3].

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

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[2].
Bromfenac (0.032-3.16%; 100 μL; rubbed onto the paws) produces dose-related anti-inflammatory activity in rats[2].
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[2].
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[2].
Bromfenac (0.32%; 50μL; rubbed onto the abdomen) produces significant blockade of abdominal constriction to ACh challenge in mice[2].

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.

91714-93-1

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)

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
10 mM 0.2808 mL 1.4039 mL 2.8078 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

*All of the co-solvents are provided by MCE.
References
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Keywords:

BromfenacCOXCyclooxygenaseCOX-1COX-2NSAIDpostoperativeinflammationpaincataractCMEInhibitorinhibitorinhibit

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Bromfenac sodium
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