Bromfenac Sodium Sesquihydrate

Alias: AHR10282B; AHR 10282B
Cat No.:V16754 Purity: ≥98%
Bromfenac sodium hydrate (Bromfenac monosodium salt sesquihydrate) is a potent and orally bioactive COX inhibitor (antagonist) with IC50s of 5.56 and 7.45 nM for COX-1 and COX-2, respectively.
Bromfenac Sodium Sesquihydrate Chemical Structure CAS No.: 120638-55-3
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
10mg
50mg
100mg
Other Sizes

Other Forms of Bromfenac Sodium Sesquihydrate:

  • Bromfenac Sodium (AHR 10282R)
  • Bromfenac
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
Bromfenac sodium hydrate (Bromfenac monosodium salt sesquihydrate) is a potent and orally bioactive COX inhibitor (antagonist) with IC50s of 5.56 and 7.45 nM for COX-1 and COX-2, respectively. Bromfenac sodium hydrate may be utilized to study ocular inflammation.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
In a concentration-dependent manner, bromfenac (0-80 μg/mL; 24 h) suppresses the epithelial-to-mesenchymal transition of HLEC-B3 caused by transforming growth factor-β2 [2]. The transforming growth factor-β2-induced epithelial-to-mesenchymal transition in the human anterior capsule is inhibited by bromfenac (80 μg/Ml; 48 h) [2].
ln Vivo
In rats, bromfenac (0.0032-3.16%; 100 or 200 μL; applied to the back) demonstrated notable antibacterial action at doses as low as 0.1% (4 hours prior to treatment) or 0.32% (18 hours prior to treatment). an increase in inflammation [3]. In rats, the application of 100 μL of bromfenac (0.032-3.16%) results in dose-dependent anti-inflammatory effects [3]. When administered directly to guinea pigs' UV-exposed skin regions, bromfenac (0.032-1.0%; 50 μL) was 26 times more effective than indomethacin at preventing erythema [3]. Rats' paw volume of both hindlimbs decreases in a dose- and time-dependent manner when bromfenac (0.0032-0.1%; 50 μL) is administered to the uninjected paw four hours a day, five days a week [3]. When administered topically to the abdomen, bromfenac (0.32%; 50 μL) dramatically prevents belly contractions in mice given acetylcholine [3]. When applied twice daily for four weeks, 1 μL (0.09%) of bromfenac eye drops per eye partially lowers corneal staining, which slows down after four weeks [4].
Cell Assay
Cell viability assay[2]
Cell Types: Transforming growth factor-β2-treated human anterior capsule
Tested Concentrations: 80 μg/mL
Incubation Duration: 48 hrs (hours)
Experimental Results: Transforming growth factor-β2-induced epithelial-mesenchymal transition was inhibited in primary LECs .

Cell migration assay[2]
Cell Types: HLEC-B3 Cell
Tested Concentrations: 0, 20, 40, 60 and 80 μg/mL
Incubation Duration: 24 hrs (hours)
Experimental Results: Inhibition of transforming growth factor-β2-induced cell migration in HLEC-B3 cells, and demonstrated inhibition of overexpression of epithelial-mesenchymal transition markers.
Animal Protocol
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats (150-250 g) injected with carrageenan [3]
Doses: 0.0032, 0.01, 0.032, 0.1, 0.32, 1.0, 3.16% (100 or 200 μL)
Route of Administration: 1 Carrageenan injected on back - 72 hrs (hrs (hours)) before injection
Experimental Results: Significant anti-inflammatory activity was produced when applied at 0.32% 1, 2 and 4 hrs (hrs (hours)) before carrageenan challenge. Carrageenan is effective when applied 1 or 4 hrs (hrs (hours)) before challenge, but not 0.2% when applied 24 hrs (hrs (hours)) (or more) before challenge.

Animal/Disease Models: Male injected with Salin or BTX-B[4]
Doses: 1 μL (0.09%) per eye
Route of Administration: eye drops; 1 μL (0.09%) per eye; twice a day; 4-week
Experimental Results: Corneal fluorescein staining scores improved 4 weeks after treatment.
References
[1]. Tetsuo Kida, et al. Pharmacokinetics and efficacy of topically applied nonsteroidal anti-inflammatory drugs in retinochoroidal tissues in rabbits. PLoS One. 2014 May 5;9(5):e96481.
[2]. Xiaobo Zhang, et al. Drug-eluting intraocular lens with sustained bromfenac release for conquering posterior capsular opacification. Bioact Mater. 2021 Jul 23;9:343-357.
[3]. Nolan JC, et, al. The topical anti-inflammatory and analgesic properties of bromfenac in rodents. Agents Actions. 1988 Aug; 25(1-2): 77-85.
[4]. Kaevalin Lekhanont, et al. Effects of topical anti-inflammatory agents in a botulinum toxin B-induced mouse model of keratoconjunctivitis sicca. J Ocul Pharmacol Ther. 2007 Feb;23(1):27-34.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C30H28BR2N2NA2O9
Molecular Weight
766.35
CAS #
120638-55-3
Related CAS #
Bromfenac sodium;91714-93-1;Bromfenac;91714-94-2
SMILES
[O-]C(CC1=CC=CC(C(C2=CC=C(Br)C=C2)=O)=C1N)=O.[Na+].[1.5H2O]
Synonyms
AHR10282B; AHR 10282B
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ≥ 100 mg/mL (~260.98 mM)
H2O : ≥ 100 mg/mL (~260.98 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: 33.33 mg/mL (86.98 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.3049 mL 6.5244 mL 13.0489 mL
5 mM 0.2610 mL 1.3049 mL 2.6098 mL
10 mM 0.1305 mL 0.6524 mL 1.3049 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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