1. Immunology/Inflammation Apoptosis
  2. COX Apoptosis
  3. Diclofenac potassium

Diclofenac potassium 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 potassium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.

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Diclofenac potassium Chemical Structure

Diclofenac potassium Chemical Structure

CAS No. : 15307-81-0

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Based on 12 publication(s) in Google Scholar

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Description

Diclofenac potassium 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 potassium 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 nM (IC50)

Ovine COX-1

5.1 nM (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.

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

334.24

Formula

C14H10Cl2KNO2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O[K])CC1=CC=CC=C1NC2=C(Cl)C=CC=C2Cl

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 : 100 mg/mL (299.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 14.29 mg/mL (42.75 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9919 mL 14.9593 mL 29.9186 mL
5 mM 0.5984 mL 2.9919 mL 5.9837 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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 (7.48 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 (7.48 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
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
H2O / DMSO 1 mM 2.9919 mL 14.9593 mL 29.9186 mL 74.7966 mL
5 mM 0.5984 mL 2.9919 mL 5.9837 mL 14.9593 mL
10 mM 0.2992 mL 1.4959 mL 2.9919 mL 7.4797 mL
15 mM 0.1995 mL 0.9973 mL 1.9946 mL 4.9864 mL
20 mM 0.1496 mL 0.7480 mL 1.4959 mL 3.7398 mL
25 mM 0.1197 mL 0.5984 mL 1.1967 mL 2.9919 mL
30 mM 0.0997 mL 0.4986 mL 0.9973 mL 2.4932 mL
40 mM 0.0748 mL 0.3740 mL 0.7480 mL 1.8699 mL
DMSO 50 mM 0.0598 mL 0.2992 mL 0.5984 mL 1.4959 mL
60 mM 0.0499 mL 0.2493 mL 0.4986 mL 1.2466 mL
80 mM 0.0374 mL 0.1870 mL 0.3740 mL 0.9350 mL
100 mM 0.0299 mL 0.1496 mL 0.2992 mL 0.7480 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • 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.

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