中文名称:

(2-氨基-3-(4-溴苯甲酰)苯基)乙酸钠

中文同义词:

溴酚酸钠;溴芬那酸钠水合物;溴芬酸钠水合物;溴芬酸钠;溴芬那酸钠;(2-氨基-3-(4-溴苯甲酰)苯基)乙酸钠;(2-氨基-3-(4-溴苯甲酰)苯基)乙酸钠水合物;溴芬酸钠120638-55-3

英文名称:

Bromfenac Sodium Sesquihydrate

英文同义词:

Sodium (2-amino-3-(4-bromobenzoyl)phenyl)acetate;Benzeneacetic acid, 2-amino-3-(4-bromobenzoyl)-, monosodium salt, hydrate (2:3);Bromfenac ophthalmic;Bromfenac ophthalmic solution;Duract;Sodium 2-amino-3-(4-bromobenzoyl) phenylacetate sesquihydrate;Unii-8ecv571Y37;Bromfenac monosodium salt sesquihydrate

CAS号:

120638-55-3

分子式:

C15H11BrNNaO3

分子量:

356.15

EINECS号:

695-342-6

相关类别:

眼科用药;医药 眼科用药;小分子抑制剂;有机原料;小分子抑制剂，天然产物;医药原料;Intermediates Fine Chemicals;Pharmaceuticals;Inhibitors;原料药

Mol文件:

120638-55-3.mol

熔点 

268-270°C (dec.)

储存条件 

Refrigerator

生物活性

Bromfenac sodium hydrate (Bromfenac monosodium salt sesquihydrate) 是一种有效的和具有口服活性的 COX 抑制剂，抑制 COX-1 和 COX-2 的 IC50 值分别为 5.56 和 7.45 nM。Bromfenac sodium hydrate 是一种溴化非甾体类抗炎/镇痛药 (NSAID)，通常用于白内障手术后的术后炎症和疼痛以及假晶状体囊状黄斑水肿 (CME) 的研究。

靶点

COX-1 5.56 nM (IC 50 ) COX-2 7.45 nM (IC 50 )

COX-1 5.56 nM (IC 50 )

COX-2 7.45 nM (IC 50 )

体外研究

Bromfenac (90 μg/mL; 48 h) inhibits TGF-b1-induced extracellular matrix (ECM) synthesis and myofibroblast activation in HConFs and HPFs. Bromfenac (30-90 μg/mL; 48 h) decreases the protein and mRNA expression levels of FN, COL3, a-SMA, and survivin in a dose-dependent manner in HConFs and HPFs. Bromfenac (30-90 μg/mL; 48 h) declines the phosphorylated protein levels of AKT, ERK1/2, and GSK-3b-S9 with dosage in HPFs and HConFs.

体内研究

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. Bromfenac (0.032-3.16%; 100 μL; rubbed onto the paws) produces dose-related anti-inflammatory activity in rats. 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. 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. Bromfenac (0.32%; 50μL; rubbed onto the abdomen) produces significant blockade of abdominal constriction to ACh challenge in mice. Animal Model: Male Sprague-Dawley rats (150-250 g) are injected carrageenan 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 Sprague-Dawley rats (150-250 g) are injected carrageenan

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%.