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Purity: ≥98%
Bromfenac Sodium (formerly AHR-10282R; AHR10282R; AHR-10282, AHR10282; trade names Prolensa, Bromday, Xibrom), an approved nonsteroidal anti-inflammatory drug (NSAID), is an orally bioavailable COX-1/2 inhibitor with anti-inflammatory activity. It can inhibit the biosynthesis of prostaglandin by blocking cyclooxygenase 1 and 2.
| ln Vitro |
In HLEC-B3, bromfenac (0-80 μg/mL; 24 h) can block the epithelial-mesenchymal transition triggered by transforming growth factor-β2 in a concentration-dependent way[2]. In human anterior capsules, the transforming growth factor-β2-induced epithelial-mesenchymal transition is inhibited by bromfenac (80 μg/Ml; 48 h)[2].
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| ln Vivo |
In rats, bromfenac (0.0032-3.16%; 100 or 200 μL; applied topically) has notable anti-inflammatory effects at doses as low as 0.1% (4 hours before treatment) or 0.32% (18 hours before treatment)[3]. When applied topically to the paws, bromfenac (0.032-3.16%; 100 μL) has dose-dependent anti-inflammatory effects in rats[3]. Applying bromfenac (0.032-1.0%; 50 μL) directly to the skin area of guinea pigs exposed to UV light is 26 times more effective than indomethacin at preventing erythema[3]. The amount of paw volume in both hind limbs of rats is reduced in a dose and time dependent manner when bromfenac (0.0032-0.1%; 50 μL) is rubbed onto the uninjected paw for four hours a day, five days a week[3]. When applied topically to the abdomen, bromfenac (0.32%; 50 μL) significantly inhibits mice's abdominal constriction in response to an ACh challenge[3]. When applied as eyedrops, 1 μL (0.09%) of bromfenac is applied twice daily for four weeks, partially reducing corneal staining, which becomes less noticeable by the fourth week[4].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: transforming growth factor-β2-treated human anterior capsules. Tested Concentrations: 80 μg/mL Incubation Duration: 48 hrs (hours) Experimental Results: Suppressed transforming growth factor-β2-induced epithelial-mesenchymal transition in primary lens epithelial cells (LECs). Cell Migration Assay [2] Cell Types: HLEC-B3 cells Tested Concentrations: 0, 20, 40, 60, and 80 μg/ mL Incubation Duration: 24 hrs (hours) Experimental Results: Suppressed transforming growth factor-β2-induced cell migration in HLEC-B3 cells, and demonstrated inhibition of the over-expression of epithelial-mesenchymal transition markers. |
| Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats (150-250 g) are injected carrageenan[2]
Doses: 0.0032, 0.01, 0.032, 0.1, 0.32, 1.0, 3.16% (100 or 200 μL) Route of Administration: Rubbed onto the backs before 1-72 h of injected carrageenan Experimental Results: 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 carrageenan challenge at 0.2%. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Milk levels of bromfenac are likely to be low with the usual oral dosage, but milk levels have not been measured after higher injectable dosages. Use caution when using bromfenac in nursing mothers, especially with the injectable drug. Maternal use of bromfenac eye drops would not be expected to cause any adverse effects in breastfed infants. To substantially diminish the amount of drug that reaches the breastmilk after using eye drops, place pressure over the tear duct by the corner of the eye for 1 minute or more, then remove the excess solution with an absorbent tissue. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References |
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| Additional Infomation |
Bromfenac sodium salt is the sodium salt of bromfenac. Note that 'bromfenac sodium' commonly refers to the sesquihydrate (120638-55-3); this is the anhydrous form. It has a role as a non-steroidal anti-inflammatory drug and a non-narcotic analgesic. It contains a bromfenac(1-).
Bromfenac Sodium is the sodium salt form of bromfenac, a nonsteroidal anti-inflammatory drug (NSAID) with analgesic and anti-inflammatory activities. Upon ophthalmic administration, bromfenac binds to and inhibits the activity of cyclooxygenase II (COX II), an enzyme which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins (PG). By inhibiting PG formation, bromfenac is able to inhibit PG-induced inflammation, thereby preventing vasodilation, leukocytosis, disruption of the blood-aqueous humor barrier, an increase in vascular permeability and an increase in intraocular pressure (IOP). See also: Bromfenac (has active moiety). Drug Indication Treatment of postoperative ocular inflammation following cataract extraction in adults. |
| Molecular Formula |
C15H11BRNO3.NA
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| Molecular Weight |
356.15
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| Exact Mass |
354.981
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| CAS # |
91714-93-1
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| Related CAS # |
Bromfenac sodium hydrate;120638-55-3;Bromfenac;91714-94-2;Bromfenac-d4 sodium;2749400-35-7
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| PubChem CID |
23693301
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| Appearance |
Light yellow to yellow solid powder
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| Boiling Point |
562.2ºC at 760 mmHg
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| Melting Point |
285ºC
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| Flash Point |
293.8ºC
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| Vapour Pressure |
1.77E-13mmHg at 25°C
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| LogP |
2.135
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
21
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| Complexity |
372
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
HZFGMQJYAFHESD-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C15H12BrNO3.Na/c16-11-6-4-9(5-7-11)15(20)12-3-1-2-10(14(12)17)8-13(18)19;/h1-7H,8,17H2,(H,18,19);/q;+1/p-1
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| Chemical Name |
2-Amino-3-(4-bromobenzoyl)benzeneacetic acid sodium
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
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| 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 Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.14 mg/mL (3.20 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 11.4 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 1.14 mg/mL (3.20 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 11.4 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05107921 | Recruiting | Drug: Bromfenac Sodium | Familial Exudative Vitreoretinopathies | Seoul National University Hospital | November 1, 2021 | Phase 2 |
| NCT01387464 | Completed Has Results | Drug: ISV-303 Drug: Bromday™ |
Cataract | Sun Pharmaceutical Industries Limited | July 2011 | Phase 2 |
| NCT01576952 | Completed Has Results | Drug: ISV-303 Other: DuraSite Vehicle |
Ocular Inflammation | Sun Pharmaceutical Industries Limited | July 2012 | Phase 3 |
| NCT01310127 | Completed Has Results | Drug: Bromfenac Drug: Nepafenac |
Inflammation Pseudophakia |
Toyos Clinic | November 2010 | Phase 4 |
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