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120638-55-3

中文名稱 (2-氨基-3-(4-溴苯甲酰)苯基)乙酸鈉
英文名稱 Bromfenac Sodium Sesquihydrate
CAS 120638-55-3
分子式 C15H11BrNNaO3
分子量 356.15
MOL 文件 120638-55-3.mol
更新日期 2024/10/28 09:57:21
120638-55-3 結(jié)構(gòu)式 120638-55-3 結(jié)構(gòu)式

基本信息

中文別名
溴芬酸鈉
溴酚酸鈉
溴芬那酸鈉
溴芬酸鈉水合物
溴芬那酸鈉水合物
溴芬酸鈉120638-55-3
(2-氨基-3-(4-溴苯甲酰)苯基)乙酸鈉
(2-氨基-3-(4-溴苯甲酰)苯基)乙酸鈉水合物
(2-氨基-3-(4-溴苯甲酰)苯基)乙酸鈉倍半水合物
英文別名
Duract
Unii-8ecv571Y37
Bromfenac sodiu
Bromfenac ophthalmic
acetate hydrate(2:2:3)
Bromfenac sodium hydrate
BroMfenac sodiuM 1.5H2O
Sodium bromfenate hydrate
Bromfenac ophthalmic solution
Bromfenac Sodium Sesquihydrate
所屬類別
原料藥:眼科用藥

物理化學(xué)性質(zhì)

熔點(diǎn)268-270°C (dec.)
儲(chǔ)存條件Refrigerator
溶解度DMSO: ≥ 100 mg/mL (260.98 mM); Water: ≥ 100 mg/mL (260.98 mM)
形態(tài)Solid
顏色Light yellow to yellow

安全數(shù)據(jù)

警示詞危險(xiǎn)
危險(xiǎn)性描述H372-H300

常見(jiàn)問(wèn)題列表

生物活性
Bromfenac sodium hydrate (Bromfenac monosodium salt sesquihydrate) 是一種有效的和具有口服活性的 COX 抑制劑,抑制 COX-1 和 COX-2 的 IC50 值分別為 5.56 和 7.45 nM。Bromfenac sodium hydrate 是一種溴化非甾體類抗炎/鎮(zhèn)痛藥 (NSAID),通常用于白內(nèi)障手術(shù)后的術(shù)后炎癥和疼痛以及假晶狀體囊狀黃斑水腫 (CME) 的研究。
靶點(diǎn)

COX-1

5.56 nM (IC 50 )

COX-2

7.45 nM (IC 50 )

體外研究

Bromfenac (90 μg/mL; 48 h) inhibits TGF-b1-induced extracellular matrix (ECM) synthesis and myo?broblast 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.

體內(nèi)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%.
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