Product Introduction
Bioactivity


英文名: Bromfenac

描述: Bromfenac 可用于研究眼部的炎症，它是一种强效的、口服有效的COX 抑制剂，对 COX-1 和 COX-2 的IC50值分别为 5.56 和 7.45 nM。

体外活性: 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 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.

体内活性: 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%; 50μL; 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%; 50μL; 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year