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15307-86-5

中文名称 双氯芬酸
英文名称 1-(2,6-Dichlorophenyl)-2-indolinone
CAS 15307-86-5
EINECS 编号 239-348-5
分子式 C14H9Cl2NO
MDL 编号 MFCD00451393
分子量 278.13
MOL 文件 15307-86-5.mol
更新日期 2024/03/25 13:53:25
15307-86-5 结构式 15307-86-5 结构式

基本信息

中文别名
双氯芬酸
奥尔芬
2-[(2,6-二氯苯基)氨基]-苯乙酸
英文别名
1-(2,6-DICHLOROPHENYL)-1,3-DIHYDRO-INDOLE-2-ONE
(N-1-(2,6-DICHLOROPHENYL) -2-INDOLIN-2-ONE
Diciofenac
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
dichlofenac
[2-(2,6-Dichloroanilino)phenyl]-acetic acid
2-[2-(2,6-Dichlorophenyl)aminophenyl]ethanoic acid
Diclofenac
DICLOFENAC FREE ACID
Rhumalgan
2-(2-(2,6-dichlorophenylamino)phenyl)acetic acid
所属类别
原料药:非甾抗炎药

物理化学性质

熔点156-158°
沸点412.0±45.0 °C(Predicted)
密度1.431±0.06 g/cm3(Predicted)
储存条件Sealed in dry,Room Temperature
溶解度溶于甲醇
酸度系数(pKa)pKa 4 (Uncertain)
形态粉末晶体
颜色白色到近乎白色
水溶解性1.278mg/L(30 ºC)
Merck14,3081
InChIKeyDCOPUUMXTXDBNB-UHFFFAOYSA-N

安全数据

危险性符号(GHS)
GHS06,GHS08,GHS09
警示词危险
危险性描述H301-H361d-H372-H411
危险品运输编号3249
RTECS号AG6310000
海关编码2922.49.2600
危险等级6.1(b)
包装类别III

应用领域

用途一
用作消炎镇痛药

常见问题列表

简介
双氯芬酸商品名有扶他林、待克菲那、服他灵等,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、痛风,以及偏头痛、牙痛、胆结石和肾结石等需要急性止痛的情况。药用双氯芬酸常使用钠盐或钾盐,在中国主要以钠盐为主,即双氯芬酸钠,各个国家的情况各有不同。
?作用机理

双氯芬酸的作用机理为抑制环氧化酶活性,从而阻断花生四烯酸向前列腺素的转化生成,因前列腺素为引起疼痛、发烧及发炎等之现象的主要因子。

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 )

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.
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).
双氯芬酸价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/01/25HY-15036双氯芬酸
Diclofenac
15307-86-5500mg350元
2024/01/25HY-15036双氯芬酸
Diclofenac
15307-86-55G484元
2024/01/25HY-15036双氯芬酸
Diclofenac
15307-86-510mM * 1mLin DMSO500元
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