Licensed by Pfizer Catalog No.S1576 Synonyms: Azulfidine
Molecular Weight(MW): 398.39
Sulfasalazine is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis.
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|Description||Sulfasalazine is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis.|
Sulfasalazine, like methotrexate, enhances adenosine release at an inflamed site and that adenosine diminishes inflammation via occupancy of A2 receptors on inflammatory cells.  Sulfasalazine treatment for 4 hours inhibits kappaB-dependent transcription with an IC50 value of approximately 0.625 mM. Sulfasalazine (2.5 mM) results in cell death of T-lymphocytes in a dose- and time-dependent manner. Sulfasalazine but not 5ASA or sulfapyridine, strongly inhibits NF-kappaB activation and potently induces apoptosis in T-lymphocytes.  Sulfasalazine is cleaved into sulfapyridine and 5-aminosalicylic acid (5-ASA; mesalamine) by colonic bacteria, and the latter, too, is reported to suppress NF-kappaB activity. Sulfasalazine but not its cleaved form 5-ASA causes a dose-dependent inhibition of glioma growth, this effect is entirely attributable to the inhibition of cystine uptake via the system x(c)(-) cystine-glutamate transporter. Sulfasalazine inhibits cystine uptake causing a chronic depletion of intracellular GSH and consequently compromised cellular redox defense which stymied tumor growth. 
|In vivo||Sulfasalazine markedly decreases the number of leukocytes that accumulated in the inflamed (carrageenan, 2 mg/ml) air pouch in the murine air pouch model of inflammation. Sulfasalazine treatment promotes a marked increase in splenocyte 5-aminoimidazole-4-carboxamidoribonucleotide (AICAR) concentration, which is consistent with the in vitro observation that sulfasalazine inhibits AICAR transformylase. |
|In vitro||DMSO||80 mg/mL (200.8 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02930343||Recruiting||Rheumatoid Arthritis||Jawaharlal Institute of Postgraduate Medical Education & Research||September 2016||Phase 4|
|NCT02374021||Recruiting||Arthritis, Rheumatoid||Brigham and Womens Hospital|Columbia University||July 2016||Phase 4|
|NCT03012763||Completed||Pharmacokinetics|Magnetic Resonance Imaging|Administration, Oral||University Medicine Greifswald||April 2016||Phase 1|
|NCT02638896||Not yet recruiting||Ankylosing Spondylitis||Zhixiang Huang|Health and Family Planning Commission of Guangdong||January 2016||Phase 4|
|NCT02434861||Completed||Chemotherapy-induced Nausea and Vomiting||Tesaro, Inc.||May 2015||Phase 1|
|NCT02373202||Completed||Rheumatoid Arthritis||Sanofi|Regeneron Pharmaceuticals||February 2015||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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