Home Neuronal Signaling COX inhibitor Diclofenac Sodium For research use only.

Diclofenac Sodium

Synonyms: GP 45840

Diclofenac Sodium (GP 45840) is a non-selective COX inhibitor with IC50 of 0.5 μg/ml and 0.5 μg/ml for COX-1 and -2 in intact cells, respectively, used as a nonsteroidal anti-inflammatory drug (NSAID) to relieve pain and reduce swelling in flammation.

Diclofenac Sodium Chemical Structure

Diclofenac Sodium Chemical Structure

CAS No. 15307-79-6

Purity & Quality Control

Diclofenac Sodium Related Products

Signaling Pathway

COX Signaling Pathways

COX Signaling Pathway

Biological Activity

Description Diclofenac Sodium (GP 45840) is a non-selective COX inhibitor with IC50 of 0.5 μg/ml and 0.5 μg/ml for COX-1 and -2 in intact cells, respectively, used as a nonsteroidal anti-inflammatory drug (NSAID) to relieve pain and reduce swelling in flammation.
Targets
COX-1 [1] COX-2 [1]
60 nM 200 nM
In vitro
In vitro Diclofenac inhibits Wnt/beta-catenin signaling without altering the level of beta-catenin protein and reduces the expression of beta-catenin/TCF-dependent genes. Diclofenac induces the degradation of IkappaBalpha, which increases free nuclear factor kappaB (NF-kappaB) in colon cancer cells. [1] Diclofenac suppresses both fast tetrodotoxin-sensitive (TTX-S) and the slow tetrodotoxin-resistant (TTX-R) sodium currents in a dose-dependent manner. Diclofenac produces shifts of the steady-state inactivation curves in the hyperpolarizing direction in both types of sodium currents in a dose-dependent manner. Diclofenac may bind to sodium channels with a greater affinity when they are in the inactivated state than when they are in the resting state. [2] Diclofenac results in a severe accumulation of protein in the tubular cells (so called hyaline droplet degeneration), macrophage infiltration and structural alterations (dilation, vesiculation) of the endoplasmic reticulum (ER) in the proximal and distal renal tubules of kidney. Diclofenac also results in shortening of podocytes and their retraction from the basal lamina, a thickening of the basal lamina, the formation of desmosomes, and necrosis of endothelial cells in the renal corpuscles of kidney. [3]
In Vivo
In vivo Diclofenac (0.01 to 0.2 mM) stimulates state-4 respiration and slightly inhibits state 3 in rats, decreasing the respiratory control ratio, while the membrane potential is decreased or collapsed (depending on the drug concentration). [4]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06053411 Not yet recruiting
Interaction
Washington State University
 January 1 2024 Early Phase 1
NCT06146491 Recruiting
Pain Postoperative
B.P. Koirala Institute of Health Sciences
 August 10 2023 Phase 4
NCT05968482 Active not recruiting
Healthy
Amzell
 July 11 2023 Phase 1
NCT05752526 Active not recruiting
Dysmenorrhea Primary
Daré Bioscience Inc.
 May 19 2023 Phase 1

Chemical Information & Solubility

Molecular Weight 318.13 Formula

C14H10Cl2NNaO2
CAS No. 15307-79-6 SDF Download Diclofenac Sodium SDF
Smiles C1=CC=C(C(=C1)CC(=O)[O-])NC2=C(C=CC=C2Cl)Cl.[Na+]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 64 mg/mL ( (201.17 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 64 mg/mL

Water : 14 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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