Bromfenac sodium hydrate (Bromfenac monosodium salt sesquihydrate) 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 sodium hydrate 可用于眼部炎症研究。
| 生物活性 | Bromfenac sodium hydrate (Bromfenac monosodium salt sesquihydrate) is a potent and orally active inhibitor ofCOX, withIC50s of 5.56 and 7.45 nM forCOX-1andCOX-2, respectively. Bromfenac sodium hydrate can be used in ocular inflammation research[1]. |
| IC50& Target[1] | COX-1 5.56 nM (IC50) | 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 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%; 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(260.98 mM) H2O : ≥ 100 mg/mL(260.98 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.6098 mL | 13.0490 mL | 26.0981 mL | | 5 mM | 0.5220 mL | 2.6098 mL | 5.2196 mL | | 10 mM | 0.2610 mL | 1.3049 mL | 2.6098 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 33.33 mg/mL (86.98 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.52 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.52 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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