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100mg | ||
250mg | ||
500mg |
ln Vitro |
In a concentration-dependent manner, bromfenac (0-80 μg/mL; 24 h) inhibits the epithelial-to-mesenchymal transition of HLEC-B3 induced by transforming growth factor-β2 [2]. In the human anterior capsule, the transforming growth factor-β2-induced epithelial-to-mesenchymal transition is inhibited by bromfenac (80 μg/mL; 48 h) [2].
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ln Vivo |
Rats treated with a solution of bromfenac (0.0032-3.16%; 100 or 200 μL; rubbed on the back) showed notable antimicrobial activity at concentrations as low as 0.1% (4 hours before treatment) or 0.32% (18 hours before treatment). inflammation [3]. When applied topically to the paws of rats, bromfenac (0.032-3.16%; 100 μL) exhibits dose-dependent anti-inflammatory effects [3]. Applying bromfenac (0.032-1.0%; 50 μL) directly to guinea pigs' UV-exposed skin areas inhibited erythema 26 times more effectively than indomethacin [3]. Both the dose and the duration of the application of bromfenac (0.0032-0.1%; 50 μL) to the uninjected paw of rats results in a dose- and time-dependent reduction in the volume of the hindlimbs [3]. When administered topically to the abdomen of mice challenged with acetylcholine, bromfenac (0.32%; 50 μL) significantly inhibits abdominal contractions [3]. During the 4-week period, bromfenac (eye drops; 1 μL (0.09%) per eye; twice daily) slows down and partially reduces corneal staining [4].
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Cell Assay |
Cell Viability Assay[2]
Cell Types: Human anterior capsule treated with transforming growth factor-β2 Tested Concentrations: 80 μg/mL Incubation Duration: 48 hrs (hours) Experimental Results: Inhibition of transforming growth factor-β2-induced epithelial- mesenchymal transition (LEC). 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. |
Molecular Formula |
C15H12NO3BR
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Molecular Weight |
334.16468
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CAS # |
91714-94-2
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Related CAS # |
Bromfenac sodium;91714-93-1;Bromfenac sodium hydrate;120638-55-3
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SMILES |
O=C(O)CC1=CC=CC(C(C2=CC=C(Br)C=C2)=O)=C1N
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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)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.9926 mL | 14.9629 mL | 29.9258 mL | |
5 mM | 0.5985 mL | 2.9926 mL | 5.9852 mL | |
10 mM | 0.2993 mL | 1.4963 mL | 2.9926 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.
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.
(2) Be sure to add the solvent(s) in order.