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)
