Diclofenac Sodium

Catalog No.S1903 Synonyms: GP 45840

Diclofenac Sodium Chemical Structure

Molecular Weight(MW): 318.13

Diclofenac Sodium 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.

Size Price Stock Quantity  
In DMSO USD 90 In stock
USD 70 In stock
USD 210 In stock
USD 470 In stock
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Biological Activity

Description Diclofenac Sodium 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
Synonyms GP 45840

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02985671 Not yet recruiting Postural Low Back Pain|Mechanical Low Back Pain Ache Laboratorios Farmaceuticos S.A. June 2017 Phase 3
NCT03020368 Recruiting Rhizarthrosis Charite University, Berlin, Germany January 2017 --
NCT02952898 Recruiting Actinic Keratosis Gage Development Company, LLC October 2016 Phase 3
NCT02714699 Not yet recruiting Endoscopy Assiut University September 2016 Phase 2|Phase 3
NCT02918812 Recruiting Female Infertility of Tubal Origin Bayer University Kano, Nigeria September 2016 Phase 4
NCT02837770 Completed Pain University Hospital of Patras July 2016 --

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COX Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID