双氯芬酸

双氯芬酸用途

Diclofenac 是一种有效的,非选择性的抗炎剂,为 COX 的抑制剂,在 CHO 细胞中,对人 COX-1 和 COX-2 的 IC50 值分别为 4 nM,1.3 nM；Diclofenac 同时对绵羊 COX-1 和 COX-2 的 IC50 值分别为 5.1 μM,0.84 μM。

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双氯芬酸名称

[ CAS 号 ]:
15307-86-5

[ 中文名 ]:
双氯芬酸

[ 英文名 ]:
Diclofenac

[中文别名 ]:

2-(2,6-二氯苯氨基)苯乙酸

[英文别名 ]:

2-{2-[(2,6-dichlorophenyl)amino]phenyl}acetic acid
Benzeneacetic acid, 2-((2,6-dichlorophenyl)amino)-
2-(2-((2,6-dichlorophenyl)amino)phenyl)acetic acid
Acetic acid, (o-(2,6-dichloroanilino)phenyl)-
2-[[2,6-Dichlorophenyl]amino]benzeneacetic acid
MFCD00451393
2-((2,6-dichlorophenyl)amino)benzeneacetic acid
Diclofenac acid
2-[2-[(2,6-dichlorophenyl)amino]phenyl]acetic acid
N-(2,6-Dichlorophenyl)-o-aminophenylacetic Acid

双氯芬酸生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 免疫及炎症 >> COX

研究领域 >> 炎症/免疫

[ 靶点 ]

Human COX-2:1.3 nM (IC50, in CHO cells)

Human COX-1:4 nM (IC50, in CHO cells)

Ovine COX-2:0.84 μM (IC50)

Ovine COX-1:5.1 μM (IC50)

[体外研究]

双氯芬酸是一种有效的COX抑制剂,CHO细胞中人COX-1和COX-2的IC50分别为4 nM和1.3 nM。双氯芬酸有效阻断UX37细胞微粒体中COX-1介导的前列腺素产生,IC50为7±3 nM [1]。双氯芬酸钠表现出对COX-1和COX-2酶的抑制作用,IC50分别为5.1和0.84μM[2]。

[体内研究]

双氯芬酸(3mg/kg,bid,5天)显着增加大鼠粪便51Cr排泄,并且在施用1mg/kg每天两次,持续4天后,在松鼠猴中也观察到这种效果[1]。双氯芬酸(10mg/kg)在小鼠中显示出抗炎活性[2]。双氯芬酸(10 mg/kg)可降低氧化低密度脂蛋白(Ox-LDL),但通过肌内注射大鼠对过氧化氢酶和谷胱甘肽过氧化物酶的动力学参数没有影响[3]。

[动物实验]

大鼠[1]雄性Sprague-Dawley大鼠（150±200g）口服给予双氯芬酸一次（急性给药）或每天两次，持续5天（慢性给药）。在第4天早晨剂量后1小时获得血浆样品，用于测量双氯芬酸浓度。在第5天给予最后一次剂量后，立即通过尾静脉向大鼠注射来自供体大鼠的0.5mL 51Cr标记的红细胞，其与51铬酸钠一起孵育。将大鼠单独置于代谢笼中，随意食物和水。收集粪便48小时，51Cr粪便排泄量计算为总注射剂量的百分比（每只动物20mCi）[1]。松鼠猴[1]松鼠猴（Saimiri sciureus; 0.8±1.4 kg）口服双氯芬酸，每日两次，持续1±5天。给予最后一剂后1小时，通过隐静脉注射51CrCl3的无菌盐水（1mL / kg，每只动物4±5mCi），并获得血浆样品用于测量双氯芬酸浓度。然后将猴子单独圈养在代谢笼中。收集粪便24小时，51Cr粪便排泄量计算为总注射剂量的百分比[1]。

[参考文献]

[1]. Riendeau D, et al. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor. Br J Pharmacol. 1997 May;121(1):105-17.

[2]. Labib MB, et al. Design, synthesis of novel isoindoline hybrids as COX-2 inhibitors: Anti-inflammatory, analgesic activities and docking study. Bioorg Chem. 2018 Oct;80:70-80.

[3]. Curcelli EC, et al. Beneficial effects of diclofenac therapy on serum lipids, oxidized low-density lipoprotein and antioxidant defenses in rats. Life Sci. 2008 Apr 9;82(15-16):892-8.

[相关活性小分子]

双氯芬酸物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
412.0±45.0 °C at 760 mmHg

[ 熔点 ]:
156-158ºC

[ 分子式 ]:
C₁₄H₁₁Cl₂NO₂

[ 分子量 ]:
296.149

[ 闪点 ]:
203.0±28.7 °C

[ 精确质量 ]:
295.016693

[ PSA ]:
49.33000

[ LogP ]:
4.06

[ 外观性状 ]:
白色至淡黄色结晶粉末

[ 蒸汽压 ]:
0.0±1.0 mmHg at 25°C

[ 折射率 ]:
1.662

[ 储存条件 ]:
室温，干燥

[ 水溶解性 ]:
可溶于：甲醇

双氯芬酸MSDS

详细MSDS(安全技术说明书)

双氯芬酸毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: AG6310000

CHEMICAL NAME :: Acetic acid, (o-(2,6-dichloroanilino)phenyl)-

CAS REGISTRY NUMBER :: 15307-86-5

LAST UPDATED :: 199612

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C14-H11-Cl2-N-O2

MOLECULAR WEIGHT :: 296.16

WISWESSER LINE NOTATION :: QV1R BMR BG FG

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 1070 ug/kg

TOXIC EFFECTS :: Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200 Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year: 117,1058,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 62500 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,1398,1980

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 170 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: PHARAT Pharmazie. (VEB Verlag Volk und Gesundheit, Neue Gruenstr. 18, Berlin DDR-1020, Ger. Dem. Rep.) V.1- 1946- Volume(issue)/page/year: 37,148,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 345 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 43,44,1993 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 4 mg/kg

SEX/DURATION :: female 13 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

REFERENCE :: JCGBDF Journal of Craniofacial Genetics and Developmental Biology. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1980- Volume(issue)/page/year: 10,83,1990

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 4 mg/kg

SEX/DURATION :: female 13 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

REFERENCE :: JCGBDF Journal of Craniofacial Genetics and Developmental Biology. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1980- Volume(issue)/page/year: 10,83,1990

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双氯芬酸安全信息

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
3249

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2942000000

双氯芬酸合成路线

详细合成路线

双氯芬酸上下游产品

双氯芬酸上游产品

双氯芬酸下游产品

双氯芬酸海关

[ 海关编码 ]: 2922499990

[ 中文概述 ]:
2922499990 其他氨基酸及其酯及它们的盐（含有一种以上含氧基的除外）. 增值税率:17.0% 退税率:9.0% 监管条件:AB(入境货物通关单,出境货物通关单) 最惠国关税:6.5% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乙醇胺及其盐应报明色度, 乙醇胺及其盐应报明包装

[ 监管条件 ]: A.入境货物通关单 B.出境货物通关单

[ 检验检疫 ]: P.进境动植物、动植物产品检疫 Q.出境动植物、动植物产品检疫 R.进口食品卫生监督检验 S.出口食品卫生监督检验 M.进口商品检验 N.出口商品检验

[ Summary ]:
HS:2922499990 other amino-acids, other than those containing more than one kind of oxygen function, and their esters; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:AB(certificate of inspection for goods inward,certificate of inspection for goods outward) MFN tariff:6.5% General tariff:30.0%

双氯芬酸相关知识

[双氯芬酸]-说明书-作用-双氯芬酸钠缓释片副作用

2019-01-14 16:18:51

导读：双氯芬酸（通用名英语：Diclofenac，来自于其化学名2-(2,6-dichloranilino) phenylacetic acid ），商品名如扶他林，是一种衍生于苯乙酸类的非甾体抗炎药（NSAID），主要用于治疗骨关节炎、类风湿关节炎、多发性肌炎、皮肌炎、脊柱关节病、强直性脊柱炎、...