Bromfenac 是一种强效且具有口服活性的COX抑制剂，对 COX-1 和 COX-2 的IC50分别为 5.56 和 7.45 nM。Bromfenac 可用于眼部炎症研究。
| 生物活性 | Bromfenac is a potent and orally active inhibitor ofCOX, withIC50s of 5.56 and 7.45 nM forCOX-1andCOX-2, respectively. Bromfenac can be used in ocular inflammation research[1]. |
| IC50& Target | Human COX-1 5.56 nM (IC50) | Human COX-2 7.45 nM (IC50) |
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体外研究
(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].
Cell Viability Assay[2] | Cell Line: | Transforming growth factor-β2-treated human anterior capsules | | Concentration: | 80 μg/mL | | Incubation Time: | 48 hours | | Result: | Suppressed transforming growth factor-β2-induced epithelial-mesenchymal transition in primary lens epithelial cells (LECs). |
Cell Migration Assay[2] | Cell Line: | HLEC-B3 cells | | Concentration: | 0, 20, 40, 60, and 80 μg/mL | | Incubation Time: | 24 hours | | 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. |
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体内研究
(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[3].
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].
| Animal Model: | Male Sprague-Dawley rats (150-250 g) are injected carrageenan[3] | | 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%. |
| Animal Model: | Male injected with Salin or BTX-B[4] | | Dosage: | 1 μL (0.09%) per eye | | Administration: | Eyedrop instillation; 1 μL (0.09%) per eye; twice-daily; 4 weeks | | Result: | Improved the corneal fluorescein staining score later at 4 weeks after treatment. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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