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Purity: ≥98%
Sulfasalazine (NSC-667219) is an approved antiinflammatory drug used for the treatment of rheumatoid arthritis, inflammatory bowel disease such as including ulcerative colitis and Crohn's disease. It has been claimed that sulfasalazine can stop NF-κB activity. In comparison to other DMARDs, it is frequently well tolerated. Sulfasalazine has been shown to reverse the scarring linked to liver cirrhosis in clinical trials for the treatment of chronic alcoholics.
| Targets |
NF-κB; COX-2; TGF-β; RelA; Autophagy
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| ln Vitro |
Sulfasalazine treatment prevents NFκB activation brought on by TNFα, LPS, or phorbol ester in SW620 colon cells. Sulfasalazine inhibits NFκB-dependent transcription at micro- to millimolar concentrations. Through the inhibition of IB degradation, sulfasalazine prevents TNFα-induced nuclear translocation of NFκB[1]. All pro-inflammatory cytokines have their basal mRNA expression levels significantly increased by pre-incubation with 5 mM sulfasalazine alone, with IL-6 mRNA levels increasing by 80 times when compared to vehicle control[2]. Colonic bacteria break down sulfasalazine after digestion to produce sulfapyridine and 5-aminosalicylic acid, both of which have been shown to inhibit NF-kappaB activity[3].
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| ln Vivo |
The amount of leukocytes that accumulated in the inflamed (carrageenan, 2 mg/ml) air pouch in the murine air pouch model of inflammation is significantly reduced by sulfasalazine. It is consistent with the in vitro finding that sulfasalazine inhibits AICAR transformylase that sulfasalazine treatment leads to a significant increase in splenocyte 5-aminoimidazole-4-carboxamidoribonucleotide (AICAR) concentration.
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| Cell Assay |
In the culture medium, sulfasalazine is dissolved. In addition to glutamine, 10% heat-inactivated FCS, and 1% (wt/vol) penicillin/streptomycin, SW620 cells are grown in Dulbecco's modified Eagle medium. The 3xIgkBLuc reporter construct is transfected into SW620 cells. Prior to stimulation with TNFα, LPS, or PMA, cells are first allowed to rest for 18 hours with either medium alone or sulfasalazine (0.1, 0.2, 0.5, 1, 2, 5 mM). The luciferase assay is carried out[1].
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| Animal Protocol |
Mice: Sulfasalazine is dissolved in 0.1 M NaOH and neutralized by titrating with 0.1 M HCl. A SCID mouse's head is implanted with U-87MG glioma cells. Animals are randomly divided into three groups of five after seven days. For three weeks, one group is given twice-daily 1 mL intraperitoneal saline injections. The two test groups are given 8 mg of sulfasalazine in 1 mL of saline twice daily for three weeks. Animal health and tumor growth were observed. Mouse brains were removed, rinsed, and put in 30% sucrose after being perfused with 4% paraformaldehyde[3].
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| References |
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| Molecular Formula |
C18H14N4O5S
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|---|---|
| Molecular Weight |
398.3926
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| Exact Mass |
398.07
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| Elemental Analysis |
C, 54.27; H, 3.54; N, 14.06; O, 20.08; S, 8.05
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| CAS # |
599-79-1
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| Related CAS # |
Sulfasalazine-d4;1346606-50-5
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| Appearance |
Light yellow to orange solid powder
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| LogP |
3.18
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| tPSA |
149.69
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| SMILES |
InChI=1S/C18H14N4O5S/c23-16-9-6-13(11-15(16)18(24)25)21-20-12-4-7-14(8-5-12)28(26,27)22-17-3-1-2-10-19-17/h1-11,23H,(H,19,22)(H,24,25)
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| InChi Key |
NCEXYHBECQHGNR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H14N4O5S/c23-16-9-6-13(11-15(16)18(24)25)21-20-12-4-7-14(8-5-12)28(26,27)22-17-3-1-2-10-19-17/h1-11,23H,(H,19,22)(H,24,25)
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| Chemical Name |
NCEXYHBECQHGNR-UHFFFAOYSA-N
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| Synonyms |
NSC-667219; NSC 667219; NSC667219; NSC203730; NSC-203730; NSC 203730; Sulfasalazine; Reupirin; Rorasul; Azopyrin
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~80 mg/mL(~200.8 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.28 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 10 mg/mL (25.10 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5101 mL | 12.5505 mL | 25.1010 mL | |
| 5 mM | 0.5020 mL | 2.5101 mL | 5.0202 mL | |
| 10 mM | 0.2510 mL | 1.2551 mL | 2.5101 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06060301 | Active Recruiting |
Drug: sulfasalazine 500 MG Drug: corticosteroids |
Oral Lichen Planus Corticosteroids |
Cairo University | March 1, 2023 | Phase 3 |
| NCT05703425 | Recruiting | Drug: Sulfasalazine | Preterm Birth | Rutgers, The State University of New Jersey |
March 1, 2023 | Phase 2 |
| NCT03847311 | Recruiting | Drug: Sulfasalazine Drug: Placebos |
Breast Cancer Chronic Pain Due to Malignancy (Finding) |
University of Arizona | May 3, 2021 | Phase 2 |
| NCT03561584 | Recruiting | Drug: Sulfasalazine Drug: Placebo |
Primary Sclerosing Cholangitis | Brigham and Women's Hospital | July 1, 2018 | Phase 2 |
| NCT05580861 | Not yet recruiting | Drug: Sulfasalazine Ph | Acute Myeloid Leukemia | Assistance Publique - Hôpitaux de Paris |
February 2023 | Phase 1 Phase 2 |
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