2. Immunology/Inflammation Apoptosis
  3. COX Apoptosis
  4. Diclofenac diethylamine

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.

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Diclofenac diethylamine Chemical Structure

Diclofenac diethylamine Chemical Structure

CAS No. : 78213-16-8

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Based on 16 publication(s) in Google Scholar

Other Forms of Diclofenac diethylamine:

Diclofenac diethylamine Related Antibodies

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  • Biological Activity

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Description

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[1], and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively[2]. Diclofenac diethylamine induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade[3].

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)

In Vitro

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.

Diclofenac diethylamine Related Antibodies

Cell Viability Assay[3]

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[3]

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.
In Vivo

Diclofenac (3 mg/kg, b.i.d., for 5 days) significantly increases faecal 51Cr excretion in rats, and such effect is also observed in squirrel monkeys after administrated of 1 mg/kg twice daily for 4 days[1].
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.

Animal Model: Male Sprague-Dawley rats (150±200 g)[1]
Dosage: 3 mg/kg
Administration: Oral administration, b.i.d., for 5 days
Result: Resulted in a significant increase in faecal 51Cr excretion.
Animal Model: Wistar rats (150-175 g) bearing Formalin-induced rat foot paw edema model[2]
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).
Clinical Trial
Molecular Weight

369.29

Formula

C18H22Cl2N2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CC1=CC=CC=C1NC2=C(Cl)C=CC=C2Cl.CCNCC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7079 mL 13.5395 mL 27.0790 mL
5 mM 0.5416 mL 2.7079 mL 5.4158 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.96%

COA (254 KB) LCMS (265 KB)

Handling Instructions (2659 KB)
References

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
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Diclofenac diethylamine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Diclofenac78213-16-8COXApoptosisCyclooxygenaseanti-inflammatoryCOX-1COX-2CHOovineneuralstemcellsNSCscaspasecascadeInhibitorinhibitorinhibit

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