Diclofenac Sodium

For research use only.

Catalog No.S1903 Synonyms: GP 45840

3 publications

Diclofenac Sodium Chemical Structure

CAS No. 15307-79-6

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.

Selleck's Diclofenac Sodium has been cited by 3 publications

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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

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 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]

Protocol

Solubility (25°C)

In vitro DMSO 64 mg/mL (201.17 mM)
Ethanol 64 mg/mL (201.17 mM)
Water 14 mg/mL (44.0 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 318.13
Formula

C14H10Cl2NNaO2

CAS No. 15307-79-6
Storage powder
in solvent
Synonyms GP 45840
Smiles C1=CC=C(C(=C1)CC(=O)[O-])NC2=C(C=CC=C2Cl)Cl.[Na+]

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03150732 Not yet recruiting Drug: Systemic nalbuphine|Drug: Local nalbuphine Postoperative Pain Assiut University December 10 2021 Not Applicable
NCT05026320 Recruiting Drug: Naproxen gel|Drug: Diclofenac gel|Drug: Placebo gel Soft Tissue Injury Bayer|Deutsche Sporthochschule Köln August 8 2021 Phase 2
NCT04530903 Recruiting Drug: Clonidine|Drug: Levobupivacaine|Drug: NaCl 0.9% Proctological Surgery Centre Hospitalier Universitaire Saint Pierre September 9 2020 Phase 4

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COX Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID