双氯芬酸

中文名称:

双氯芬酸

中文同义词:

2-(2,6-二氯苯氨基)苯乙酸;2-[(2,6-二氯苯基)氨基]-苯乙酸;奥尔芬;双氯芬酸;双氯芬酸钠杂质D;双氯芬酸 10G;双氯芬酸 标准品;双氯芬酸溶液,100PPM

英文名称:

1-(2,6-Dichlorophenyl)-2-indolinone

英文同义词:

Diciofenac;1-(2,6-DICHLOROPHENYL)-1,3-DIHYDRO-INDOLE-2-ONE;(N-1-(2,6-DICHLOROPHENYL) -2-INDOLIN-2-ONE;2-[[2,6-Dichlorophenyl] amino] benzeneacetic acid;1-(2,6-DICHLOROPHENYL)-2-INDOLINONE /MEQUITAZINE;1-(2,6-DICHLOROPHENYL)-2-INDOLINONE/INDOLINONE;DICLOFENAC ACID/[2-(2,6-DICHLORO-PHENYLAMINO)-PHENY]-ACETIC ACID;(o-(2,6-dichloroanilino)phenyl)-acetic acid

CAS号:

15307-86-5

分子式:

C14H11Cl2NO2

分子量:

296.15

EINECS号:

239-348-5

相关类别:

医药化工类;原料中间体-原料药;原料药API;医药原料;解热镇痛类;酶抑制剂;双氯芬酸钠中间体;其他兽药标准品;中间体;小分子抑制剂;强效消炎镇痛;化合物：原料药：解热镇痛类;抗炎镇痛药物;原料;主打;医药原料药;医药、农药及染料中间体;有机化工原料;Indoles and derivatives;pharmacetical

Mol文件:

15307-86-5.mol

熔点 

156-158°

沸点 

412.0±45.0 °C(Predicted)

密度 

1.431±0.06 g/cm3(Predicted)

酸度系数(pKa)

pKa 4 (Uncertain)

水溶解性 

1.278mg/L(30 ºC)

Merck 

14,3081

InChIKey

DCOPUUMXTXDBNB-UHFFFAOYSA-N

CAS 数据库

15307-86-5(CAS DataBase Reference)

NIST化学物质信息

Benzeneacetic acid, 2-[(2,6-dichlorophenyl)amino]-(15307-86-5)

EPA化学物质信息

Benzeneacetic acid, 2-[(2,6-dichlorophenyl)amino]- (15307-86-5)

性质

双氯芬酸为白色结晶性粉末，无臭，易溶于丙酮，溶于甲，乙醇，微溶于水。

药理作用

双氯芬酸具有显著的抗风湿，消炎，止痛和解热作用，其抗炎作用比阿司匹林强26—50倍，能很好的解除关节疼能，消肿，改善其活动，同时具有良好的耐受性。

生物活性

Diclofenac acid是一种非类固醇的消炎药，具有止痛、消炎和退热活性，在治疗多种急性和慢性疼痛、炎症反应中有效。它能抑制cyclooxygenase-1 (COX-1)和cyclooxygenase-2 (COX-2)，具有相近的效力。

靶点

Human COX-2 1.3 nM (IC 50 , in CHO cells) Human COX-1 4 nM (IC 50 , in CHO cells) Ovine COX-2 0.84 μM (IC 50 ) Ovine COX-1 5.1 μM (IC 50 )

Human COX-2 1.3 nM (IC 50 , in CHO cells)

Human COX-1 4 nM (IC 50 , in CHO cells)

体外研究

Diclofenac effectively blocks COX-1 mediated prostanoid production from U937 cell microsomes, with an IC 50 of 7±3 nM. Diclofenac (1-60 μM; 1 day) induces neural stem cells (NSCs)death in a concentration-dependent manner. Diclofenac (10-60 μM; 6 hours) increases the expression of cleaved (activated) caspase-3. Cell Viability Assay Cell Line: Neural stem cells (NSCs) Concentration: 1, 3, 10, 30, 60 μM Incubation Time: 1 day Result: Induction of cell death was concentration-dependent and the effect was not saturated at a concentration of up to 60 μM. Western Blot Analysis Cell Line: Neural stem cells (NSCs) Concentration: 10, 30 or 60 μM Incubation Time: 6 hours Result: The activation of caspase-3 was increased in a concentration-dependent manner.

Cell Line:

Neural stem cells (NSCs)

Concentration:

1, 3, 10, 30, 60 μM

Incubation Time:

1 day

Result:

Induction of cell death was concentration-dependent and the effect was not saturated at a concentration of up to 60 μM.

Cell Line:

Neural stem cells (NSCs)

Concentration:

10, 30 or 60 μM

Incubation Time:

6 hours

Result:

The activation of caspase-3 was increased in a concentration-dependent manner.

体内研究

Diclofenac (3 mg/kg, b.i.d., for 5 days) significantly increases faecal 51 Cr excretion in rats, and such effect is also observed in squirrel monkeys after administrated of 1 mg/kg twice daily for 4 days. Diclofenac (10 mg/kg; administered via oral route just prior to induction of inflammation) shows in vivo anti-inflammatory activity in Wistar rats. Animal Model: Male Sprague-Dawley rats (150±200 g) Dosage: 3 mg/kg Administration: Oral administration, b.i.d., for 5 days Result: Resulted in a significant increase in faecal 51 Cr excretion. Animal Model: Wistar rats (150-175 g) bearing Formalin-induced rat foot paw edema model Dosage: 10 mg/kg Administration: Administered via oral route just prior to induction of inflammation Result: Showed in vivo anti-inflammatory activity (% edema inhibition=29.2, 1 h; 22.2, 3 h; 20, 6 h).

Animal Model:

Male Sprague-Dawley rats (150±200 g)

Dosage:

3 mg/kg

Administration:

Oral administration, b.i.d., for 5 days

Result:

Resulted in a significant increase in faecal 51 Cr excretion.

Animal Model:

Wistar rats (150-175 g) bearing Formalin-induced rat foot paw edema model

Dosage:

10 mg/kg

Administration:

Administered via oral route just prior to induction of inflammation

Result:

Showed in vivo anti-inflammatory activity (% edema inhibition=29.2, 1 h; 22.2, 3 h; 20, 6 h).

用途 

用作消炎镇痛药

危险品运输编号 

3249

RTECS号

AG6310000

HazardClass 

6.1(b)

PackingGroup 

III

毒害物质数据

15307-86-5(Hazardous Substances Data)