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抑制剂/激动剂
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/ Diclofenac Diethylamine/双氯芬酸二乙胺盐

Diclofenac Diethylamine/双氯芬酸二乙胺盐 {[allProObj[0].p_purity_real_show]}

货号：A115940 同义名： 双氯芬酸二乙胺 / Diclofenac (diethylamine)

Diclofenac Diethylamine是一种非选择性 COX 抑制剂，IC50 分别为 4 nM 和 1.3 nM（对 COX-1 和 COX-2）。它通过活化 caspase 级联反应诱导神经干细胞凋亡。

Diclofenac Diethylamine/双氯芬酸二乙胺盐 化学结构 CAS号：78213-16-8
Diclofenac Diethylamine/双氯芬酸二乙胺盐 化学结构
CAS号：78213-16-8
Diclofenac Diethylamine/双氯芬酸二乙胺盐 3D分子结构
CAS号：78213-16-8
Diclofenac Diethylamine/双氯芬酸二乙胺盐 化学结构 CAS号：78213-16-8
Diclofenac Diethylamine/双氯芬酸二乙胺盐 3D分子结构 CAS号：78213-16-8
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Diclofenac Diethylamine/双氯芬酸二乙胺盐 纯度/质量文件 产品仅供科研

货号：A115940 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
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• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
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产品名称 COX ↓ COX-1 ↓ COX-2 ↓ 其他靶点 纯度
Piroxicam ✔ 98%
Salicylic acid ✔ 98%
Phenacetin ✔ 98%
Etodolac ✔ 99%
Flunixin meglumine ✔ 98%
Ibuprofen L-lysine ✔ 98%
Nabumetone ✔ 98%
Acemetacin ✔ 98%
Diflunisal ✔ 98%
Pranoprofen ✔ 98%
Ampiroxicam ✔ 98%
Meloxicam ✔ 98%
Sulindac ✔ 98%
Ketoprofen ✔ 98%
Mefenamic Acid ✔ 95%
Bromfenac sodium ✔ 98%
Oxaprozin ✔ 99%
Aspirin ✔ 99%
Nepafenac ✔ 98%
Zaltoprofen ✔ 99%
Salicin ✔ 98%
Suprofen ✔ 99%+
Xanthohumol ✔ 99%
Parecoxib ✔ 98%
Tolfenamic Acid +++

COX-2, IC50: 0.2 μM

 		98%
Etoricoxib ✔ 99%
Niflumic Acid ✔ 98%
Valdecoxib ++++

COX-2, IC50: 5 nM

 		99+%
Ibuprofen +

COX-1, IC50: 13 μM

 		+

COX-2, IC50: 370 μM

 		98%
Indomethacin ++

COX1, IC50: 0.28 μM

 		+

COX-2, IC50: 14 μM

 		97%
Lornoxicam ++++

COX-1, IC50: 5 nM

 		++++

COX-2, IC50: 8 nM

 		98%
Meclofenamic acid sodium ++++

COX-1, IC50: 40 nM

 		+++

COX-2, IC50: 50 nM

 		99%
Asaraldehyde ✔ 98%
Naproxen +

COX-1, IC50: 8.7 μM

 		+

COX-2, IC50: 5.2 μM

 		98%
Diclofenac Sodium Salt +++

COX-1, IC50: 60 nM

 		+++

COX-2, IC50: 200 nM

 		98%
NS-398 ++

COX-2, IC50: 3.8 μM

 		95%
Amfenac Sodium Hydrate ++

COX-1, IC50: 250 nM

 		+++

COX-2, IC50: 150 nM

 		98%+
Nimesulide +

COX-2, IC50: 26 μM

 		98%
Lumiracoxib ++

COX-1, Ki: 3 μM

 		+++

COX-2, Ki: 60 nM

 		98%
Rutaecarpine ✔ 95%
Celecoxib ++++

COX-2, IC50: 40 nM

 		98%
Carprofen ++++

canine COX2, IC50: 30 nM

 		98%
Ketorolac ++

COX-1 (human), IC50: 1.23 μM

 		++

COX-2 (human), IC50: 3.50 μM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Diclofenac Diethylamine/双氯芬酸二乙胺盐 生物活性

描述 Diclofenac diethylamine acts as a potent and nonselective anti-inflammatory agent by inhibiting both COX-1 and COX-2, with IC50 values of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells[1]. Diclofenac diethylamine triggers apoptosis in neural stem cells (NSCs) by activating the caspase cascade[3].
体内研究

Diclofenac (3 mg/kg, b.i.d., for 5 days) significantly elevates faecal 51Cr excretion in rats. A similar effect is observed in squirrel monkeys when administered 1 mg/kg twice daily for 4 days[1].

Diclofenac (10 mg/kg) demonstrates anti-inflammatory activity in Wistar rats in vivo[1].
体外研究

Diclofenac effectively inhibits the production of COX-1 mediated prostanoids from U937 cell microsomes, exhibiting an IC50 of 7±3 nM[1].

Diclofenac (1-60 μM; 1 day) triggers the death of neural stem cells (NSCs)[3].

Diclofenac (10-60 μM) upregulates the expression of cleaved (activated) caspase-3 within 6 hours[3].

Diclofenac Diethylamine/双氯芬酸二乙胺盐 细胞实验

Cell Line
Concentration Treated Time Description References
L3.7 cells 1 μM inhibited CD73 expression, reduced migration and invasion Adv Sci (Weinh). 2023 Feb;10(6):e2206335.
PANC-1 cells 1 μM inhibited CD73 expression, reduced migration and invasion Adv Sci (Weinh). 2023 Feb;10(6):e2206335.
Mouse primary hepatocytes 300 µM 24 h Diclofenac-induced lipid accumulation was confirmed in mouse primary hepatocytes. Theranostics. 2022 Feb 21;12(5):2351-2369.
HepG2 cells 0.5 mM 24 h To test the effect of NSAIDs on neutral lipid accumulation in hepatocytes, diclofenac showed the most potency. Theranostics. 2022 Feb 21;12(5):2351-2369.
Mouse primary hepatocytes (MPH) 500 μM 24 h Diclofenac increased LC3-II, SQSTM1, and NBR1 protein levels, indicating autophagosome accumulation Redox Biol. 2020 Oct;37:101751.
HepG2 cells 500 μM 24 h Diclofenac increased LC3-II, SQSTM1, and NBR1 protein levels, indicating autophagosome accumulation Redox Biol. 2020 Oct;37:101751.
Renal primary proximal tubule cells (RPTCs) 400 μM 24 h To evaluate the cytotoxicity of diclofenac on RPTCs and the protective effect of cilastatin. Results showed cilastatin mitigated diclofenac-induced cytotoxicity by inhibiting mitochondrial damage. Br J Pharmacol. 2020 May;177(9):1933-1948.
HEK293 cells 10 μM 10 min To investigate OAT1/3-mediated transport and cytotoxicity of diclofenac and its glucuronide metabolite. Results showed that diclofenac acyl glucuronide, but not diclofenac, is an OAT1/3 substrate. Br J Pharmacol. 2020 May;177(9):1933-1948.
8505c 100 µM 3 and 6 h To evaluate the effect of diclofenac on metabolic gene expression, results showed no significant effect on transcriptional regulation of HIF1A and glycolytic genes Br J Cancer. 2023 Aug;129(2):249-265.
BCPAP 50 µM and 100 µM 3, 6, and 24 h To evaluate the effect of diclofenac on metabolic gene expression, results showed no significant effect on transcriptional regulation of HIF1A and glycolytic genes Br J Cancer. 2023 Aug;129(2):249-265.

Diclofenac Diethylamine/双氯芬酸二乙胺盐 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice PDAC xenograft model Intraperitoneal 20 mg/kg Daily for 28 days Inhibited CD73 expression, reduced liver metastasis Adv Sci (Weinh). 2023 Feb;10(6):e2206335.
C57BL/6 mice Hepatic steatosis model Intraperitoneal injection 100 mg/kg Every 12 hours for 24 hours To evaluate the effect of diclofenac on hepatic lipid accumulation in mice, results showed diclofenac increased hepatic lipid accumulation. Theranostics. 2022 Feb 21;12(5):2351-2369.
C57BL/6 mice Hepatotoxicity model Intraperitoneal injection 150 or 200 mg/kg Single dose, sacrificed after 6 h Diclofenac increased serum ALT, AST, and LDH levels, and rapamycin pretreatment significantly reduced these serum biomarkers Redox Biol. 2020 Oct;37:101751.
Rats Diclofenac-induced enteropathy model Oral 10 mg/kg 6 days To investigate the effect of ciprofloxacin on the pharmacokinetics of diclofenac and its alleviation of diclofenac-induced enteropathy. Results showed that ciprofloxacin alleviated diclofenac-induced enteropathy by inhibiting intestinal β-glucuronidase activity. Acta Pharmacol Sin. 2016 Jul;37(7):1002-12
Rats Diclofenac-induced enteropathy model Intravenous 5 mg/kg 15 days To investigate the effect of ciprofloxacin on the pharmacokinetics of diclofenac and its alleviation of diclofenac-induced enteropathy. Results showed that ciprofloxacin alleviated diclofenac-induced enteropathy by inhibiting intestinal β-glucuronidase activity. Acta Pharmacol Sin. 2016 Jul;37(7):1002-12
Kunming male mice Diclofenac-induced acute kidney injury model Oral 200 mg/kg Single dose, evaluated after 24 hours To assess the protective effect of cilastatin against diclofenac-induced acute kidney injury. Results demonstrated cilastatin alleviated kidney injury by restoring redox balance, suppressing inflammation, and reducing apoptosis, while decreasing renal distribution of diclofenac and its metabolite. Br J Pharmacol. 2020 May;177(9):1933-1948.
Kunming mice Diclofenac-induced small intestinal mucosal injury model Oral gavage 2.5 mg/kg Once daily for 3 days To investigate the effect of diclofenac on small intestinal mucosal injury in mice. Results showed that diclofenac significantly increased intestinal mucosal permeability, pathological score, MDA and MPO levels, and impaired mitochondrial function. Acta Pharmacol Sin. 2011 Apr;32(4):495-502

Diclofenac Diethylamine/双氯芬酸二乙胺盐 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03434197 Osteoarthritis Knee Pain Phase 3 Recruiting September 30, 2019 Indonesia ... 展开 >> Klinik Perisai Husada Recruiting Bandung, Indonesia Contact: Laniyati Hamijoyo, Dr. Sp.PD-KR          Rumah Sakit Hasan Sadikin Recruiting Bandung, Indonesia Contact: Rachmat Gunadi Wachjudi, Dr. Sp.PD-KR          Rumah Sakit Umum Daerah Al Ihsan Bale Endah Recruiting Bandung, Indonesia Contact: Andri Reza, Dr. Sp.PD-KR          Rumah Sakit Anna Medika Bekasi Recruiting Jakarta, Indonesia Contact: Ika Wulan Yuliani, Dr. Sp.PD-KR          Rumah Sakit Islam Pd. Kopi Recruiting Jakarta, Indonesia Contact: Tanggo Meriza, Dr. Sp.PD-KR          Rumah Sakit Siloam Karawaci Recruiting Jakarta, Indonesia Contact: Sandra Sinthya Langow, Dr. Sp.PD-KR 收起 <<
NCT01335724 Neck Pain Phase 4 Completed - Germany ... 展开 >> NCH investigative site Cologne, Germany NCH investigative site Essen, Germany NCH investigative site Munich, Germany 收起 <<
NCT01335724 - Completed - -

Diclofenac Diethylamine/双氯芬酸二乙胺盐 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.

[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.

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

Diclofenac Diethylamine/双氯芬酸二乙胺盐 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.54mL

2.71mL

1.35mL

27.08mL

5.42mL

2.71mL

Diclofenac Diethylamine/双氯芬酸二乙胺盐 技术信息

CAS号78213-16-8
分子式C18H22Cl2N2O2
分子量 369.29
SMILES Code O=C(O)CC1=CC=CC=C1NC2=C(Cl)C=CC=C2Cl.CCNCC
MDL No. MFCD01862249
别名 双氯芬酸二乙胺 ;Diclofenac (diethylamine)
运输蓝冰
InChI Key ZQVZPANTCLRASL-UHFFFAOYSA-N
Pubchem ID 115087
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C
溶解方案

DMSO: 145 mg/mL(392.65 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
方案 二
方案 三

Tags: Diclofenac | 78213-16-8 | COX Inhibitor | Immunology/Inflammation | Apoptosis | COX | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Diclofenac Diethylamine/双氯芬酸二乙胺盐 纯度/质量文件 | Diclofenac Diethylamine/双氯芬酸二乙胺盐 亚型比较 | Diclofenac Diethylamine/双氯芬酸二乙胺盐 生物活性 | Diclofenac Diethylamine/双氯芬酸二乙胺盐 临床数据 | Diclofenac Diethylamine/双氯芬酸二乙胺盐 参考文献 | Diclofenac Diethylamine/双氯芬酸二乙胺盐 实验方案 | Diclofenac Diethylamine/双氯芬酸二乙胺盐 技术信息

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