Zileuton sodium
Based on 26 publication(s) in Google Scholar
Zileuton sodium (A 64077 sodium) is a potent and selective inhibitor of 5-lipoxygenase, exhibiting inflammatory activities.
For research use only. We do not sell to patients.
- Purity : 98.66%
- CAS No.: 118569-21-4
- Formula: C11H11N2NaO2S
- Molecular Weight:258.27
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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HY-14398
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HY-N2056
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HY-14164
Zileuton5-Lipoxygenase Inhibitor -
HY-13750
EbselenVDCC Inhibitor -
HY-A0060
Malotilate5-LOX Inhibitor -
HY-12341
Onvoloxastat12-LOX Inhibitor -
HY-103157
PD14617615-LO Inhibitor -
HY-14166
MK-886FLAP Inhibitor -
HY-13419
U-73122Phospholipase C Inhibitor -
HY-N0892
AKBANrf2 Activator -
HY-14164R
Zileuton (Standard)5-Lipoxygenase Inhibitor -
HY-A0060R
Malotilate (Standard)5-LOX Inhibitor
Publications Citing Use of MedChemExpress (MCE) Zileuton sodium
More- Nat Commun. 2024 Sep 10;15(1):7914. [Abstract]
- Sci Immunol. 2026 May;11(119):eadz0348. [Abstract]
- Redox Biol. 2024 May:71:103096. [Abstract]
- MedComm (2020). 2026 Apr 9;7(4):e70722. [Abstract]
- Cell Death Dis. 2025 May 19;16(1):403. [Abstract]
- J Neuroinflammation. 2025 Aug 28;22(1):208. [Abstract]
- J Cachexia Sarcopenia Muscle. 2022 Aug;13(4):2242-2253. [Abstract]
- ACS Environ Au. 2025 Aug 5;5(6):573-582. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- Emerg Microbes Infect. 2022 Dec;11(1):1806-1818. [Abstract]
- J Ethnopharmacol. 2023 Jun 12:309:116357. [Abstract]
- Int J Mol Sci. 2022 Apr 28;23(9):4910. [Abstract]
- Front Cell Infect Microbiol. 2022 Feb 4;12:825824. [Abstract]
- Food Chem (Oxf). 2026 Jun 1:12:100426. [Abstract]
- J Cell Mol Med. 2025 Jun;29(11):e70641. [Abstract]
- Proteomics. 2018 Aug;18(15):e1700388. [Abstract]
- Toxicol Appl Pharmacol. 2026 Jun:511:117821. [Abstract]
- Biochem Biophys Res Commun. 2026 Sep 17:831:154324.
- Biochem Biophys Res Commun. 2018 Sep 3;503(1):297-303. [Abstract]
- J Toxicol Environ Health A. 2026 Jun 29:1-10. [Abstract]
- Head Neck. 2025 Feb;47(2):504-516. [Abstract]
- Northwestern University. 2026.
- University of Padua. 2024.
- bioRxiv. 2024 Jul 7:2024.07.04.601620. [Abstract]
- Oxid Med Cell Longev. 2022 Feb 9;2022:4295208. [Abstract]
- Oxid Med Cell Longev. 2019 Nov 3:2019:7536803. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
Biological Activity
Description
IC50 & Target
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5-Lipoxygenase |
In Vitro
In anti-CD3-treated cells, IL-2 decreases in Zileuton sodium (A 64077 sodium)-treated and untreated cells with increasing incubation time. Zileuton sodium (A 64077 sodium) likely reduces IL-2 levels by inhibiting 5-lipoxygenase, hence leukotriene B4 production, an IL-2 inducer[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Zileuton sodium (A 64077 sodium) (1200 mg/kg) inhibits the polyp formation in APCΔ468 colon and small intestine. Zileuton treatment inhibits the proliferation rates of non epithelial cells in polyps, and increases the apoptosis rates in polyps in rat. There is significant increase in the number of apoptotic cells in the Zileuton-treated cells both in small intestine and in the colon. The reduced proliferation rate may significantly contribute to the reduction of polyposis in both the small intestine and colon of Zileuton-fed APCΔ468 mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 118569-21-4
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Appearance Solid
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Molecular Weight 258.27
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Formula C11H11N2NaO2S
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Color White to off-white
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SMILES
CC(N([O-])C(N)=O)C1=CC2=CC=CC=C2S1.[Na+]
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Synonyms
A 64077 sodium; Abbott 64077 sodium
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (26)
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Journal Impact Factor
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Most Recent
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Nat Commun
A mouse protozoan boosts antigen-specific mucosal IgA responses in a specific lipid metabolism- and signaling-dependent manner. [Abstract]2024 Sep 10;15(1):7914. PMID: 39256385 -
Sci Immunol
2026 May;11(119):eadz0348. PMID: 42066062 -
Redox Biol
Excessive linoleic acid induces muscle oxidative stress through 5-lipoxygenase-dependent peroxidation. [Abstract]2024 May:71:103096. PMID: 38387137 -
MedComm (2020)
Ipriflavone From Aquilaria malaccensis Lam. Exosome-Like Nanoparticles Targets Prolyl Hydroxylase Domain Protein 2 (PHD2) to Enhance Hypoxia-Inducible Factor-α (HIF-α) Hydroxylation Thereby Alleviating Hypoxia-Induced Gastrointestinal Mucosal Ferroptosis. [Abstract]2026 Apr 9;7(4):e70722. PMID: 41969632 -
Cell Death Dis
A novel taxane SB-T-101141 triggers a noncanonical ferroptosis to overcome Paclitaxel resistance of breast cancer via iron homeostasis-related KHSRP. [Abstract]2025 May 19;16(1):403. PMID: 40389408 -
J Neuroinflammation
P2X7-CaMKII drives 5-LOX nuclear translocation to impair microglial function after subarachnoid hemorrhage. [Abstract]2025 Aug 28;22(1):208. PMID: 40877894 -
J Cachexia Sarcopenia Muscle
A disease-associated missense mutation in CYP4F3 affects the metabolism of leukotriene B4 via disruption of electron transfer. [Abstract]2022 Aug;13(4):2242-2253. PMID: 35686338 -
ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Emerg Microbes Infect
Gut dysbacteriosis attenuates resistance to Mycobacterium bovis infection by decreasing cyclooxygenase 2 to inhibit endoplasmic reticulum stress. [Abstract]2022 Dec;11(1):1806-1818. PMID: 35766265 -
J Ethnopharmacol
Involvement of p38 MAPK/cPLA2 and arachidonic acid metabolic pathway in Shengmai injection-induced pseudo-allergic reactions. [Abstract]2023 Jun 12:309:116357. PMID: 36906156 -
Int J Mol Sci
Zileuton, a 5-Lipoxygenase Inhibitor, Attenuates Haemolysate-Induced BV-2 Cell Activation by Suppressing the MyD88/NF-κB Pathway. [Abstract]2022 Apr 28;23(9):4910. PMID: 35563304 -
Front Cell Infect Microbiol
Dysregulation of Cytosolic c-di-GMP in Edwardsiella piscicida Promotes Cellular Non-Canonical Ferroptosis. [Abstract]2022 Feb 4;12:825824. PMID: 35186798 -
Food Chem (Oxf)
Acute plant-derived C18 fatty acid exposure was associated with changes in muscle 5-LOX protein abundance and volatile profiles in triploid rainbow trout (Oncorhynchus mykiss). [Abstract]2026 Jun 1:12:100426. PMID: 42291108 -
J Cell Mol Med
Downregulation of Alox5 Inhibits Ferroptosis to Improve Doxorubicin-Induced Cardiotoxicity via the P53/SLC7A11 Pathway. [Abstract]2025 Jun;29(11):e70641. PMID: 40485049 -
Proteomics
Integrative Analysis of Proteome and Ubiquitylome Reveals Unique Features of Lysosomal and Endocytic Pathways in Gefitinib-Resistant Non-Small Cell Lung Cancer Cells. [Abstract]2018 Aug;18(15):e1700388. PMID: 29901268
Zileuton sodium purchased from MedChemExpress. Usage Cited in: Proteomics. 2018 Aug;18(15):e1700388. [Abstract]
Comparison of Gefitinib resistant colony formation between PC9/GR cells treated with the control (DMSO) or 200uM Zileuton.
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Toxicol Appl Pharmacol
Scoparone alleviates cisplatin-induced acute kidney injury by inhibiting 5-lipoxygenase-mediated ferroptosis. [Abstract]2026 Jun:511:117821. PMID: 41967610 -
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Biochem Biophys Res Commun
Effects of intracellular iron overload on cell death and identification of potent cell death inhibitors. [Abstract]2018 Sep 3;503(1):297-303. PMID: 29890135 -
J Toxicol Environ Health A
Effect of 5-lipoxygenase protein expression in malignant breast cancer cells and mechanisms involved in tumor suppression. [Abstract]2026 Jun 29:1-10. PMID: 42370791 -
Head Neck
2025 Feb;47(2):504-516. PMID: 39290130 -
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bioRxiv
Rebalancing Viral and Immune Damage versus Tissue Repair Prevents Death from Lethal Influenza Infection. [Abstract]2024 Jul 7:2024.07.04.601620. PMID: 39372755 -
Oxid Med Cell Longev
Cepharanthine Attenuates Early Brain Injury after Subarachnoid Hemorrhage in Mice via Inhibiting 15-Lipoxygenase-1-Mediated Microglia and Endothelial Cell Ferroptosis. [Abstract]2022 Feb 9;2022:4295208. PMID: 35186185 -
Oxid Med Cell Longev
The 5-Lipoxygenase Inhibitor Zileuton Protects Pressure Overload-Induced Cardiac Remodeling via Activating PPAR α. [Abstract]2019 Nov 3:2019:7536803. PMID: 31781348
Zileuton sodium purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2019 Nov 3:2019:7536803. [Abstract]
Zileuton inhibits oxidative stress in cardiomyocytes. H9c2 cells are treated with PE (50 μM) and zileuton (100 μM) for 24 h. ROS levels in H9c2 cells (n = 6).
Zileuton sodium purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2019 Nov 3:2019:7536803. [Abstract]
Zileuton inhibits oxidative stress in cardiomyocytes. H9c2 cells are treated with PE (50 μM) and zileuton (100 μM) for 24 h. ROS levels in H9c2 cells (n = 6).
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (387.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (9.68 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (9.68 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Animal Administration[1]
Rats: Rats are randomized into 6 groups (n=12 per group): sham I/R group, I/R group, zileuton+I/R group, zileuton+indomethacin+I/R group, zileuton+ketorolac+I/R group, and zileuton+nimesulide+I/R group. 5-LOX inhibitor zileuton (5 mg/kg, orally twice daily) is given alone or with non-selective COX inhibitor indomethacin (5 mg/kg, intraperitoneally), selective COX-1 inhibitor ketorolac (10 mg/kg, orally) or selective COX-2 inhibitor nimesulide (10 mg/kg, subcutaneously). COX inhibitors are given 15 minutes before zileuton administration. All drugs are given for 3 days prior to I/R or sham I/R procedure. Dose of zileuton (5 mg/kg, twice daily) is used in this study. Rats in sham I/R group receive the vehicle of zileuton orally. Zileuton is dissolved in dimethyl sulfoxide (DMSO) and further dilutions are made using saline to achieve a final DMSO concentration of 1%.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Abueid L, et al. Inhibition of 5-lipoxygenase by zileuton in a rat model of myocardial infarction. Anatol J Cardiol. 2016 Nov 10 [Content Brief]
[2]. Kuvibidila S, et al. Hydroxyurea and Zileuton Differentially Modulate Cell Proliferation and Interleukin-2 Secretion by Murine Spleen Cells: Possible Implication on the Immune Function and Risk of Pain Crisis in Patients with Sickle Cell Disease. Ochsner [Content Brief]
[3]. Gounaris E, et al. Zileuton, 5-lipoxygenase inhibitor, acts as a chemopreventive agent in intestinal polyposis, by modulating polyp and systemic inflammation. PLoS One. 2015 Mar 6;10(3):e0121402 [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.8719 mL | 19.3594 mL | 38.7189 mL | 96.7972 mL |
| 5 mM | 0.7744 mL | 3.8719 mL | 7.7438 mL | 19.3594 mL | |
| 10 mM | 0.3872 mL | 1.9359 mL | 3.8719 mL | 9.6797 mL | |
| 15 mM | 0.2581 mL | 1.2906 mL | 2.5813 mL | 6.4531 mL | |
| 20 mM | 0.1936 mL | 0.9680 mL | 1.9359 mL | 4.8399 mL | |
| 25 mM | 0.1549 mL | 0.7744 mL | 1.5488 mL | 3.8719 mL | |
| 30 mM | 0.1291 mL | 0.6453 mL | 1.2906 mL | 3.2266 mL | |
| 40 mM | 0.0968 mL | 0.4840 mL | 0.9680 mL | 2.4199 mL | |
| 50 mM | 0.0774 mL | 0.3872 mL | 0.7744 mL | 1.9359 mL | |
| 60 mM | 0.0645 mL | 0.3227 mL | 0.6453 mL | 1.6133 mL | |
| 80 mM | 0.0484 mL | 0.2420 mL | 0.4840 mL | 1.2100 mL | |
| 100 mM | 0.0387 mL | 0.1936 mL | 0.3872 mL | 0.9680 mL |
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