1. Metabolic Enzyme/Protease
  2. Lipoxygenase
  3. Zileuton sodium

Zileuton sodium  (Synonyms: A 64077 sodium; Abbott 64077 sodium)

Cat. No.: HY-14164A Purity: 98.61%
COA Handling Instructions

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.

Zileuton sodium Chemical Structure

Zileuton sodium Chemical Structure

CAS No. : 118569-21-4

Size Price Stock Quantity
5 mg USD 38 In-stock
10 mg USD 60 In-stock
25 mg USD 99 In-stock
50 mg USD 132 In-stock
100 mg USD 228 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of Zileuton sodium:

Top Publications Citing Use of Products

    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).

    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.

    View All Lipoxygenase Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Zileuton sodium (A 64077 sodium) is a potent and selective inhibitor of 5-lipoxygenase, exhibiting inflammatory activities.

    IC50 & Target

    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

    In Zileuton sodium (A 64077 sodium) (5 mg/kg, p.o.) treated I/R rat, the effect of Zileuton to decrease NF-κB expression does not change significantly in the presence of COX inhibitors, and the group reveals significantly lower level of NF-κB staining. Zileuton (5 mg/kg, p.o.) treatment given to I/R rats decreases apoptotic index significantly. Zileuton has no significant effect on increased serum TNF-α levels in I/R group[1].
    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.

    Clinical Trial
    Molecular Weight

    258.27

    Formula

    C11H11N2NaO2S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC(N([O-])C(N)=O)C1=CC2=CC=CC=C2S1.[Na+]

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.8719 mL 19.3594 mL 38.7189 mL
    5 mM 0.7744 mL 3.8719 mL 7.7438 mL
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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.

    • Protocol 1

      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.
    • Protocol 2

      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:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: 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)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation
    References
    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%.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    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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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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