For research use only.

Licensed by Pfizer Catalog No.S1576 Synonyms: Azulfidine

2 publications

Sulfasalazine Chemical Structure

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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10mM (1mL in DMSO) USD 130 In stock
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Biological Activity

Description Sulfasalazine is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis.
In vitro

Sulfasalazine, like methotrexate, enhances adenosine release at an inflamed site and that adenosine diminishes inflammation via occupancy of A2 receptors on inflammatory cells. [1] 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. [2] 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. [3]

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. [1]


Solubility (25°C)

In vitro DMSO 80 mg/mL (200.8 mM)
Water Insoluble
Ethanol Insoluble

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Chemical Information

Molecular Weight 398.39


CAS No. 599-79-1
Storage powder
in solvent
Synonyms Azulfidine
Smiles OC(=O)C1=C(O)C=CC(=C1)N=NC2=CC=C(C=C2)[S](=O)(=O)NC3=CC=CC=N3

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03487926 Recruiting Radiation: [18F]FEPPA Major Depressive Episode|Inflammatory Bowel Diseases Centre for Addiction and Mental Health|McMaster University January 1 2019 --
NCT01577966 Completed Drug: Sulfasalazine Brain Tumor University of Alabama at Birmingham January 2012 Not Applicable
NCT01474291 Completed Biological: Tocilizumab Rheumatoid Arthritis Hoffmann-La Roche January 2012 --
NCT00637780 Terminated Drug: Sulfasalazine Arthritis Juvenile Rheumatoid Pfizer June 2010 Phase 4
NCT00356356 Completed Drug: Etanercept Ankylosing Spondylitis Amgen|Immunex Corporation April 2002 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID