Catalog No.S1903 Synonyms: GP 45840
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.
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|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.|
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.  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.  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. 
|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). |
|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.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02700815||Completed||Acute Pain||Boehringer Ingelheim||May 9 2016||Phase 3|
|NCT03221946||Completed||Orofacial Pain||Panineeya Mahavidyalaya Institute of Dental Sciences & Research Centre||January 31 2016||Phase 4|
|NCT00140972||Completed||Osteoarthritis||Merck Sharp & Dohme Corp.||December 3 2004||Phase 4|
|NCT02952898||Completed||Actinic Keratosis||Gage Development Company LLC||October 27 2016||Phase 3|
|NCT03131726||Recruiting||Graves Ophthalmopathy|Thyroid Associated Ophthalmopathy|Thyroid Associated Orbitopathy||Lund University||January 26 2018||Phase 3|
|NCT03172780||Completed||Osteoarthritis Knee||Mylan Inc.|Mylan Pharmaceuticals||May 24 2017||Phase 3|
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.
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