Bromfenac
Bromfenac 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 can be used in ocular inflammation research.
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- CAS. Nr.: 91714-94-2
- Formel: C15H12BrNO3
- Molecular Weight:334.16
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
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Human COX-1 5.56 nM (IC50) |
Human 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.
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Cell Line:Transforming growth factor-β2-treated human anterior capsules
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Concentration:80 μg/mL
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Incubation Time:48 hours
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Result:Suppressed transforming growth factor-β2-induced epithelial-mesenchymal transition in primary lens epithelial cells (LECs).
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Cell Line:HLEC-B3 cells
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Concentration:0, 20, 40, 60, and 80 μg/mL
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Incubation Time:24 hours
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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 (0.032-3.16%; 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%; 50 μL; 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%; 50 μL; 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.
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Animal Model:Male Sprague-Dawley rats (150-250 g) are injected carrageenan[3]
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Dosage:0.0032, 0.01, 0.032, 0.1, 0.32, 1.0, 3.16% (100 or 200 μL)
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Administration:Rubbed onto the backs before 1-72 h of injected carrageenan
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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%.
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Animal Model:Male injected with Salin or BTX-B[4]
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Dosage:1 μL (0.09%) per eye
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Administration:Eyedrop instillation; 1 μL (0.09%) per eye; twice-daily; 4 weeks
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Result:Improved the corneal fluorescein staining score later at 4 weeks after treatment.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 91714-94-2
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Molecular Weight 334.16
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Formel C15H12BrNO3
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SMILES
O=C(O)CC1=CC=CC(C(C2=CC=C(Br)C=C2)=O)=C1N
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Bromfenac Related Classifications
HY-B1888 Related Classifications
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