2. Metabolic Enzyme/Protease Apoptosis
  3. Lipoxygenase Ferroptosis
  4. Zileuton

Zileuton  (Synonyms: A 64077; Abbott 64077)

Cat. No.: HY-14164 Purity: 99.86%
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Zileuton is a potent and selective inhibitor of 5-lipoxygenase with antiasthmatic properties.

For research use only. We do not sell to patients.

Zileuton Chemical Structure

Zileuton Chemical Structure

CAS No. : 111406-87-2

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Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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 USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
5 mg USD 38 In-stock
10 mg USD 60 In-stock
50 mg USD 132 In-stock
100 mg USD 228 In-stock
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Customer Review

Based on 14 publication(s) in Google Scholar

Other Forms of Zileuton:

Zileuton Related Antibodies

Top Publications Citing Use of Products

    Zileuton 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 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 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:

    View All Isoforms
    5-LOX 12-LOX 15-LOX

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Zileuton is a potent and selective inhibitor of 5-lipoxygenase with antiasthmatic properties.

    IC50 & Target

    5-LOX

     

    In Vitro

    In anti-CD3-treated cells, IL-2 decreases in zileuton-treated and untreated cells with increasing incubation time. Zileuton 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.

    Zileuton Related Antibodies
    In Vivo

    In zileuton (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 (1,200 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

    236.29

    Formula

    C11H12N2O2S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC(N(O)C(N)=O)C1=CC2=CC=CC=C2S1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (423.21 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 4.2321 mL 21.1604 mL 42.3209 mL
    5 mM 0.8464 mL 4.2321 mL 8.4642 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • 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: ≥ 10 mg/mL (42.32 mM); Clear solution

      This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 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: ≥ 10 mg/mL (42.32 mM); Clear solution

      This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 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).
    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 4.2321 mL 21.1604 mL 42.3209 mL 105.8022 mL
    5 mM 0.8464 mL 4.2321 mL 8.4642 mL 21.1604 mL
    10 mM 0.4232 mL 2.1160 mL 4.2321 mL 10.5802 mL
    15 mM 0.2821 mL 1.4107 mL 2.8214 mL 7.0535 mL
    20 mM 0.2116 mL 1.0580 mL 2.1160 mL 5.2901 mL
    25 mM 0.1693 mL 0.8464 mL 1.6928 mL 4.2321 mL
    30 mM 0.1411 mL 0.7053 mL 1.4107 mL 3.5267 mL
    40 mM 0.1058 mL 0.5290 mL 1.0580 mL 2.6451 mL
    50 mM 0.0846 mL 0.4232 mL 0.8464 mL 2.1160 mL
    60 mM 0.0705 mL 0.3527 mL 0.7053 mL 1.7634 mL
    80 mM 0.0529 mL 0.2645 mL 0.5290 mL 1.3225 mL
    100 mM 0.0423 mL 0.2116 mL 0.4232 mL 1.0580 mL
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    Zileuton Related Classifications

    Help & FAQs
    • 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.

    Keywords:

    Zileuton111406-87-2A 64077 Abbott 64077A64077A-64077Abbott64077Abbott 64077Abbott-64077LipoxygenaseFerroptosisLOXInhibitorinhibitorinhibit

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