双氯芬酸

简介 ?作用机理性质药理作用生物活性靶点体外研究体内研究双氯芬酸试剂级价格

双氯芬酸

CAS号:15307-86-5
英文名:1-(2,6-Dichlorophenyl)-2-indolinone
中文名:双氯芬酸
CBNumber:CB5225367
分子式:C14H11Cl2NO2
分子量:296.15
MOL File:15307-86-5.mol

双氯芬酸化学性质

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 :soluble in Methanol
形态 :powder to crystal
酸度系数(pKa) :pKa 4 (Uncertain)
颜色 :White to Almost white
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)

安全信息

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
毒害物质数据 :15307-86-5(Hazardous Substances Data)

双氯芬酸化学药品说明书

双氯芬酸|药物应用信息
双氯芬酸缓释胶囊

双氯芬酸性质、用途与生产工艺

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).