(2-氨基-3-(4-溴苯甲酰)苯基)乙酸钠

生物活性靶点体外研究体内研究 (2-氨基-3-(4-溴苯甲酰)苯基)乙酸钠试剂级价格

CAS号:120638-55-3
英文名:Bromfenac Sodium
中文名:(2-氨基-3-(4-溴苯甲酰)苯基)乙酸钠
CBNumber:CB82130312
分子式:C15H11BrNNaO3
分子量:356.15
MOL File:120638-55-3.mol

(2-氨基-3-(4-溴苯甲酰)苯基)乙酸钠化学性质

熔点 :268-270°C (dec.)
储存条件 :Refrigerator
溶解度 :DMSO: ≥ 100 mg/mL (260.98 mM); Water: ≥ 100 mg/mL (260.98 mM)
形态 :Solid
颜色 :Light yellow to yellow

(2-氨基-3-(4-溴苯甲酰)苯基)乙酸钠性质、用途与生产工艺

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 )
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%.