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Diclofenac.

(Synonyms: 双氯芬酸)

目录号: PC14296 纯度: ≥98%

非选择性COX抑制剂，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。

CAS No. :15307-86-5

商品编号	规格	价格	会员价
PC14296-5g	5g	¥780.00	请登录
PC14296-10g	10g	¥1154.00	请登录
PC14296-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥5304.00	请登录

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中文名称

Diclofenac.

中文别名

双氯芬酸;奥尔芬,2-[(2,6-二氯苯基)氨基]-苯乙酸;2-(2,6-二氯苯氨基)苯乙酸;2-(2,6-Dichloroanilino)phenylacetic Acid 2-(2,6-二氯苯氨基)苯乙酸;醋氯芬酸杂质 A;双氯芬酸标准品;双氯芬酸钠;双氯芬酸钠杂质;双氯芬酸杂质;双氯芬酸杂质及标准品;2-[(2,6-二氯苯基)氨基]-苯乙酸;醋氯芬酸杂质A（EP）;双氯芬酸（双氯芬酸钠杂质）标准品;双氯芬酸 ;奥尔芬;双氯芬酸钠杂质D;双氯芬酸溶液,100PPM;双氯芬酸，医药级,纯度:>99%;双氯芬酸 10G

英文名称

Diclofenac

英文别名

2-(2-((2,6-Dichlorophenyl)amino)phenyl)acetic acid;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;(o-(2,6-dichloroanilino)phenyl)-acetic acid;dichlofenac;[2-(2,6-Dichloroanilino)phenyl]-acetic acid;2-[2-(2,6-Dichlorophenyl)aminophenyl]ethanoic acid;DICLOFENAC FREE ACID;Rhumalgan;2-(2-(2,6-dichlorophenylamino)phenyl)acetic acid;Diclofenac;2-(2,6-Dichloroanilino)phenylacetic Acid;4-Hydrazino-1H-pyrimidin-2-one;DICLOFENAC ACID;[2-(2,6-DICHLORO-PHENYLAMINO)-PHENY]-ACETIC ACID;1-(2,6-DICHLOROPHENYL)-2-INDOLINONE;INDOLINONE;MEQUITAZINE;Diclac;Pennsaid;Voltaflan;DicloMelan;DicloreuMa;Transfenac;Voltaren;Diclofenacum;Diclofenaco;Diclophenac;Voltarol;ProSorb-D;Novapirina;Diclofenac resinate;Cataflam;2-((2,6-Dichlorophenyl)amino)benzeneacetic acid;Diclofenacum [INN-Latin];Diclofenaco [INN-Spanish];Benzeneacetic acid, 2-[(2,6-dichlorophenyl)amino]-;Solaraze;Voltaren-XR;2-{2-[(2,6-dichlorophenyl)amino]phenyl}acetic;1-(2,6-DICHLOROPHENYL)-2-INDOLINONE /MEQUITAZINE;1-(2,6-DICHLOROPHENYL)-2-INDOLINONE/INDOLINONE;DICLOFENAC ACID/[2-(2,6-DICHLORO-PHENYLAMINO)-PHENY]-ACETIC ACID

Cas No.

15307-86-5

分子式

C₁₄H₁₁Cl₂NO₂

分子量

296.15

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

详情描述

生物活性

Diclofenac is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC₅₀s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.

性状

Solid

IC50 & Target[1][2]

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(In Vitro)

Diclofenac effectively blocks COX-1 mediated prostanoid production from U937 cell microsomes, with an IC₅₀ 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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(In Vivo)

Diclofenac (3 mg/kg, b.i.d., for 5 days) significantly increases faecal 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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 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).

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

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. [Information]

[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. [Information]

[3]. Chiho Kudo, et al. Diclofenac Inhibits Proliferation and Differentiation of Neural Stem Cells. Biochem Pharmacol. 2003 Jul 15;66(2):289-95. [Information]

溶解度数据

体外研究:

DMSO : 125 mg/mL (422.08 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.3767 mL	16.8833 mL	33.7667 mL
5 mM	0.6753 mL	3.3767 mL	6.7533 mL
10 mM	0.3377 mL	1.6883 mL	3.3767 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (7.02 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (7.02 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (7.02 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (7.02 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

搜索质检报告(COA)

产品使用指南

Data Sheet

[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. [Information]

[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. [Information]

[3]. Chiho Kudo, et al. Diclofenac Inhibits Proliferation and Differentiation of Neural Stem Cells. Biochem Pharmacol. 2003 Jul 15;66(2):289-95. [Information]

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Diclofenac.

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