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氟比洛芬,Flurbiprofen;≥98.5% (HPLC), cyclooxygenase inhibitor

别名:(±)-2-氟-α-甲基-4-联苯基乙酸;L-790330;(±)-2-Fluoro-α-methyl-4-biphenylacetic acid, L-790,330

线性分子式: C6H5C6H3(F)CH(CH3)CO2H CAS号: 5104-49-4 分子量: 244.26 EC 号: 225-827-6 MDL编号: MFCD00079303 PubChem化学物质编号: 24894968
制造商品牌: 西格玛 Sigma-Aldrich
货号(SKU): F8514
CAS号: 5104-49-4
MDL号: MFCD00079303
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¥1,133.64

说明

氟比洛芬是一种非甾体抗炎药(NSIA),具有解热、镇痛和抗真菌活性。氟比洛芬口服制剂可用于治疗类风湿性关节炎、骨关节炎和强直性脊柱炎。氟比洛芬也在眼科手术中局部使用,以预防或减少术中瞳孔缩小。氟比洛芬在结构和药理学上与布洛芬有关。它用于研究大鼠NSAID肠病的病理生理步骤以及Cunninghamella物种对氟比洛芬的生物转化。

氟比洛芬是一种环氧合酶(COX)抑制剂,是一种在前列腺素合成途径中负责花生四烯酸转化为前列腺素G2(PGG2)和PGG2转化为前列腺素H2(PGH2)的酶。这会减少导致炎症、疼痛、肿胀和发烧的前列腺素。氟比洛芬抑制COX-1和-2的活性。S对映体抑制前列腺素合成并具有抗炎和镇痛活性,而R对映体不抑制前列腺素合成,仅显示镇痛活性。

应用

Flurbiprofen is a nonsteroidal anti-inflammatory agent (NSAIA) with antipyretic, analgesic, and antifungal activity. Oral formulations of flurbiprofen may be used to treat rheumatoid arthritis, osteoarthritis and anklylosing spondylitis. Flurbiprofen is also used topically during ocular surgery to prevent or reduce intraoperative miosis. Flurbiprofen is structurally and pharmacologically related to ibuprofen. It is used to study the pathophysiological steps of NSAID enteropathy in the rat and the biotransformation of flurbiprofen by Cunninghamella species.
 

生化/生理作用

Fluibiprofen is a cyclooxygenase (COX) inhibitor, which is an enzyme responsible for the conversion of arachidonic acid to prostaglandin G2 (PGG2) and PGG2 to prostaglandin H2 (PGH2) in the prostaglandin synthesis pathway. This decreases the prostaglandins which cause inflammation, pain, swelling and fever. Flurbiprofen inhibits the activity of both COX-1 and -2. The S enantiomer inhibits prostaglandin synthesis and has both anti-inflammatory and analgesic activity, while the R enantiomer does not inhibit prostaglandin synthesis and displays only analgesic activity.
 
 

属性

生物来源

synthetic

质量水平

100

测定

≥98.5% (HPLC)

形式

powder

颜色

white to off-white

mp

110-112 °C (lit.)

溶解性

methanol: 50 mg/mL

抗生素抗菌谱

fungi

作用机制

enzyme | inhibits

SMILES string

CC(C(O)=O)c1ccc(c(F)c1)-c2ccccc2

InChI

1S/C15H13FO2/c1-10(15(17)18)12-7-8-13(14(16)9-12)11-5-3-2-4-6-11/h2-10H,1H3,(H,17,18)

InChI key

SYTBZMRGLBWNTM-UHFFFAOYSA-N

Gene Information

human ... ALB(213) , APP(351) , CYP1A2(1544) , CYP2C9(1559) , PTGS1(5742) , PTGS2(5743)
rat ... Ptgs1(24693)

 

安全信息

象形图

Skull and crossbones

警示用语:

Danger

危险声明

危险分类

Acute Tox. 3 Oral

储存分类代码

6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

WGK

WGK 3

个人防护装备

Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges

商品规格
属性名称属性值
储存温度 Storage temp.常温阴凉避光
全球实时库存 Availability √美国St. Louis ≥ 55 | 欧洲Eur. ≥ 16 | 東京Tokyo ≥ 8 | 香港与北京 ≥ 10
商品标签 [tags]