Diclofenac diethylamine
Based on 24 publication(s) in Google Scholar
Diclofenac diethylamine 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 diethylamine induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
For research use only. We do not sell to patients.
- Purity: 99.95%
- CAS No.: 78213-16-8
- Formula: C18H22Cl2N2O2
- Molecular Weight:369.29
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Diclofenac diethylamine
More- Adv Funct Mater. 2026 Feb 3.
- J Hazard Mater. 2015 May 30:289:18-27. [Abstract]
- Biomater Res. 2025 Nov 7:29:0280. [Abstract]
- Int J Biol Macromol. 2026 Mar:352:151224. [Abstract]
- Emerg Contam. 2026 Feb 23.
- Cell Rep. 2025 Feb 7;44(2):115263. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- Ecotoxicol Environ Saf. 2025 Nov 15:307:119433. [Abstract]
- J Phys Chem Solids. 2017 October;109:117-123.
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Int J Mol Sci. 2022 Oct 11;23(20):12066. [Abstract]
- Chem Biol Interact. 2021 Apr 1:338:109425. [Abstract]
- ACS Infect Dis. 2024 Aug 9;10(8):2860-2869. [Abstract]
- Pharm Res. 2022 Oct;39(10):2515-2527. [Abstract]
- Biotechnol Bioeng. 2021 Dec;118(12):4687-4698. [Abstract]
- Arch Microbiol. 2024 Jun 7;206(7):289. [Abstract]
- J Pharm Biomed Anal. 2021 Jul 15:201:114105. [Abstract]
- Phys Chem Chem Phys. 2016 Jan 21;18(3):1526-36. [Abstract]
- Toxicol Mech Methods. 2019 Nov;29(9):654-664. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2022 Sep;47(5):639-652. [Abstract]
- Thai Journal of Pharmaceutical Sciences. 2025 Dec.
- bioRxiv. 2024 Apr 7.
- Chemosphere. 2019 Jun:225:378-387. [Abstract]
- Federal University of Rio Grande do Sul. 2017 Nov.
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Bio/Physico-chemical Assay
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Cell Imaging/Staining
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Flow Cytometry
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IF
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RT-PCR
Biological Activity
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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) |
Diclofenac effectively blocks COX-1 mediated prostanoid production from U937 cell microsomes, with an IC50 of 7±3 nM[1].
Diclofenac (1-60 μM; 1 day) induces neural stem cells (NSCs)death in a concentration-dependent manner[3].
Diclofenac (10-60 μM; 6 hours) increases the expression of cleaved (activated) caspase-3[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Neural stem cells (NSCs)
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Concentration:1, 3, 10, 30, 60 μM
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Incubation Time:1 day
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Result:Induction of cell death was concentration-dependent and the effect was not saturated at a concentration of up to 60 μM.
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Cell Line:Neural stem cells (NSCs)
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Concentration:10, 30 or 60 μM
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Incubation Time:6 hours
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Result:The activation of caspase-3 was increased in a concentration-dependent manner.
Diclofenac (10 mg/kg; administered via oral route just prior to induction of inflammation) shows in vivo anti-inflammatory activity in Wistar rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (150±200 g)[1]
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Dosage:3 mg/kg
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Administration:Oral administration, b.i.d., for 5 days
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Result:Resulted in a significant increase in faecal 51Cr excretion.
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Animal Model:Wistar rats (150-175 g) bearing Formalin-induced rat foot paw edema model[2]
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Dosage:10 mg/kg
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Administration:Administered via oral route just prior to induction of inflammation
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Result:Showed in vivo anti-inflammatory activity (% edema inhibition=29.2, 1 h; 22.2, 3 h; 20, 6 h).
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 78213-16-8
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Appearance Solid
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Molecular Weight 369.29
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Formula C18H22Cl2N2O2
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Color White to off-white
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SMILES
O=C(O)CC1=CC=CC=C1NC2=C(Cl)C=CC=C2Cl.CCNCC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (24)
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Journal Impact Factor
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Most Recent
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Diclofenac diethylamine purchased from MedChemExpress. Usage Cited in: Adv Funct Mater. 2026 Feb 3.
Cumulative release of DS (Diclofenac Sodium; 50 μg/mL; 0-24 h) from HDPCK hydrogels. DS showed rapid initial release, with approximately 80% released within half a day, followed by gradual release associated with hydrogel degradation.
Diclofenac diethylamine purchased from MedChemExpress. Usage Cited in: Adv Funct Mater. 2026 Feb 3.
Intracellular ROS was visualized in chondrocytes stimulated with IL-1β and then co-cultured for 1 day with HDPC or HDPCK hydrogels containing DS (Diclofenac Sodium; 50 μg/mL); “+” groups received 808 nm NIR irradiation (0.75 W/cm²; 7 min). DS-containing hydrogels reduced intracellular ROS compared with the inflamed control group.
Diclofenac diethylamine purchased from MedChemExpress. Usage Cited in: Adv Funct Mater. 2026 Feb 3.
Chondrocyte apoptosis was analyzed by flow cytometry after IL-1β-stimulated chondrocytes were co-cultured for 1 day with HDPC or HDPCK hydrogels containing DS (Diclofenac Sodium; 50 μg/mL). DS-containing hydrogels reduced both early and late apoptosis, with the strongest effects observed in the NIR-assisted groups.
Diclofenac diethylamine purchased from MedChemExpress. Usage Cited in: Adv Funct Mater. 2026 Feb 3.
Immunofluorescence staining and semi-quantification of Col II, ACAN, and MMP13 were performed in IL-1β-stimulated chondrocytes after exposure to HDPC or HDPCK hydrogels containing DS (Diclofenac Sodium; 50 μg/mL; 1 day). DS-containing hydrogels restored Col II and ACAN expression while MMP13 was suppressed, with the most pronounced changes in the HDPCK+ group.
Diclofenac diethylamine purchased from MedChemExpress. Usage Cited in: Adv Funct Mater. 2026 Feb 3.
RT-qPCR analysis of Col II, Acan, and Mmp13 mRNA expression was performed in IL-1β-stimulated chondrocytes after exposure to HDPC or HDPCK hydrogels containing DS (Diclofenac Sodium; 50 μg/mL; 1 day). Hydrogel exposure upregulated Col II and Acan and downregulated Mmp13, with the most significant changes in the HDPCK+ group.
Diclofenac diethylamine purchased from MedChemExpress. Usage Cited in: Adv Funct Mater. 2026 Feb 3.
Western blotting was used to analyze proteins involved in inflammation-, cell metabolism-, and growth-related pathways in chondrocytes under IL-1β-induced inflammatory conditions following exposure to HDPCK or HDPCK+ hydrogels containing DS (Diclofenac Sodium; 50 μg/mL; 1 day).
Diclofenac diethylamine purchased from MedChemExpress. Usage Cited in: Adv Funct Mater. 2026 Feb 3.
H&E and Safranin O/Fast Green (SO/FG) staining of articular cartilage was performed in ACLT-induced osteoarthritis rats after intra-articular administration of HDPC or HDPCK hydrogels containing DS (Diclofenac Sodium; 50 μg/mL; i.a.; once every 2 weeks for 6 weeks). The results of H&E staining and SO/FG staining showed that the PBS group exhibited severe cartilage degeneration with significant loss of proteoglycans, whereas the treatment groups displayed effective cartilage protection.
Diclofenac diethylamine purchased from MedChemExpress. Usage Cited in: Adv Funct Mater. 2026 Feb 3.
Immunohistochemical staining and semi-quantification of Col II and ACAN were performed in ACLT-induced osteoarthritis rats after intra-articular administration of HDPC or HDPCK hydrogels containing DS (Diclofenac Sodium; 50 μg/mL; i.a.; once every 2 weeks for 6 weeks). After the incorporation of photothermal therapy and DS, articular cartilage was effectively protected.
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J Hazard Mater
Microwave-assisted activated carbon from cocoa shell as adsorbent for removal of sodium diclofenac and nimesulide from aqueous effluents. [Abstract]2015 May 30:289:18-27. PMID: 25702636 -
Biomater Res
Distinct Roles of Matrigel Enabled the Production of Expandable Hepatoblast and Polarized Hepatocyte Organoids from Human Embryonic Stem Cells under 3-Dimensional Suspension Conditions. [Abstract]2025 Nov 7:29:0280. PMID: 41209312 -
Int J Biol Macromol
Reticuline isomerase AKR1B1 with aldo-keto reductase activity and detoxification function from the insect Blaps rhynchopetera. [Abstract]2026 Mar:352:151224. PMID: 41791543 -
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Cell Rep
Spatial proteomics identifies a CRTC-dependent viral signaling pathway that stimulates production of interleukin-11. [Abstract]2025 Feb 7;44(2):115263. PMID: 39921859 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Ecotoxicol Environ Saf
PPARγ-responsive luciferase reporter system for high-throughput screening of chemical toxins with potential pulmonary fibrosis effects. [Abstract]2025 Nov 15:307:119433. PMID: 41273832 -
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Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Int J Mol Sci
Diclofenac Sensitizes Signet Ring Cell Gastric Carcinoma Cells to Cisplatin by Activating Autophagy and Inhibition of Survival Signal Pathways. [Abstract]2022 Oct 11;23(20):12066. PMID: 36292923
Diclofenac diethylamine purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Oct 11;23(20):12066. [Abstract]
KATOIII and KATO/DDP were treated with different concentration of Diclofenac (DCF) (0–1000 µM) for 48 h, and cell viability was assessed.
Diclofenac diethylamine purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Oct 11;23(20):12066. [Abstract]
The KATO/DDP cells were treated with Cisplatin alone or cisplatin in combination with Diclofenac (DCF) at 10 or 20 µM for 24 h, at 37 °C. The apoptosis cells were detected by using annexin V and PI staining and analyzed by flow cytometer.
Diclofenac diethylamine purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Oct 11;23(20):12066. [Abstract]
The combination effect of Diclofenac (DCF) (0, 5, 10, 20 μM) and Cisplatin on the expression of cleaved PARP in KATO/DDP cells was examined by Western blot analysis.
Diclofenac diethylamine purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Oct 11;23(20):12066. [Abstract]
The formation of autophagic vacuoles in KATO/DDP cells increased from 27% to 39% and 45% in cotreatments involving cisplatin and Diclofenac (DCF) at 10 and 20 μM, respectively, when compared with treatment of cisplatin alone.
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Chem Biol Interact
Regulatory effects of non-steroidal anti-inflammatory drugs on cardiac ion channels Nav1.5 and Kv11.1. [Abstract]2021 Apr 1:338:109425. PMID: 33617802 -
ACS Infect Dis
Diclofenac Sodium Restores the Sensitivity of Colistin-Resistant Gram-Negative Bacteria to Colistin. [Abstract]2024 Aug 9;10(8):2860-2869. PMID: 39073350 -
Pharm Res
Effect of Salt Form on Gelation and Drug Delivery Properties of Diclofenac-Loaded Poloxamer Gels for Delivery to Impaired Skin. [Abstract]2022 Oct;39(10):2515-2527. PMID: 36002613 -
Biotechnol Bioeng
An integrated biomimetic array chip for establishment of collagen-based 3D primary human hepatocyte model for prediction of clinical drug-induced liver injury. [Abstract]2021 Dec;118(12):4687-4698. PMID: 34478150 -
Arch Microbiol
Diclofenac sodium effectively inhibits the biofilm formation of Staphylococcus epidermidis. [Abstract]2024 Jun 7;206(7):289. PMID: 38847838 -
J Pharm Biomed Anal
A validated UHPLC-MS/MS method for simultaneous determination of lumiracoxib and its hydroxylation and acyl glucuronidation metabolites in rat plasma: Application to a pharmacokinetic study. [Abstract]2021 Jul 15:201:114105. PMID: 33991809 -
Phys Chem Chem Phys
Adsorption of sodium diclofenac on graphene: a combined experimental and theoretical study. [Abstract]2016 Jan 21;18(3):1526-36. PMID: 26671178 -
Toxicol Mech Methods
Evaluation of 3D re-cellularized tissue engineering: a drug-induced hepatotoxicity model for hepatoprotectant research. [Abstract]2019 Nov;29(9):654-664. PMID: 31345115 -
Eur J Drug Metab Pharmacokinet
Evaluation of an Ussing Chamber System Equipped with Rat Intestinal Tissues to Predict Intestinal Absorption and Metabolism in Humans. [Abstract]2022 Sep;47(5):639-652. PMID: 35733077 -
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Chemosphere
Mass-balance-model-based evaluation of sewage treatment plant contribution to residual pharmaceuticals in environmental waters. [Abstract]2019 Jun:225:378-387. PMID: 30884299 -
Solvent & Solubility
DMSO : 150 mg/mL (406.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.77 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.77 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (283 KB)
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SDS (597 KB)
- English - EN (597 KB)
- Français - FR (597 KB)
- Deutsch - DE (597 KB)
- Norwegian - NO (597 KB)
- Español - ES (597 KB)
- Swedish - SV (597 KB)
- Italian - IT (597 KB)
- Korean - KR (597 KB)
- Portuguese - PT (597 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
[3]. Chiho Kudo, et al. Diclofenac Inhibits Proliferation and Differentiation of Neural Stem Cells. Biochem Pharmacol. 2003 Jul 15;66(2):289-95. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7079 mL | 13.5395 mL | 27.0790 mL | 67.6975 mL |
| 5 mM | 0.5416 mL | 2.7079 mL | 5.4158 mL | 13.5395 mL | |
| 10 mM | 0.2708 mL | 1.3539 mL | 2.7079 mL | 6.7697 mL | |
| 15 mM | 0.1805 mL | 0.9026 mL | 1.8053 mL | 4.5132 mL | |
| 20 mM | 0.1354 mL | 0.6770 mL | 1.3539 mL | 3.3849 mL | |
| 25 mM | 0.1083 mL | 0.5416 mL | 1.0832 mL | 2.7079 mL | |
| 30 mM | 0.0903 mL | 0.4513 mL | 0.9026 mL | 2.2566 mL | |
| 40 mM | 0.0677 mL | 0.3385 mL | 0.6770 mL | 1.6924 mL | |
| 50 mM | 0.0542 mL | 0.2708 mL | 0.5416 mL | 1.3539 mL | |
| 60 mM | 0.0451 mL | 0.2257 mL | 0.4513 mL | 1.1283 mL | |
| 80 mM | 0.0338 mL | 0.1692 mL | 0.3385 mL | 0.8462 mL | |
| 100 mM | 0.0271 mL | 0.1354 mL | 0.2708 mL | 0.6770 mL |