1. Metabolic Enzyme/Protease
  2. 5-Lipoxygenase
  3. Zileuton

Zileuton (Synonyms: A 64077; Abbott 64077)

Cat. No.: HY-14164 Purity: 99.93%
Handling Instructions

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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10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
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50 mg USD 132 In-stock
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100 mg USD 228 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Zileuton:

Top Publications Citing Use of Products

    Zileuton purchased from MCE. Usage Cited in: Proteomics. 2018 Aug;18(15):e1700388.

    Comparison of Gefitinib resistant colony formation between PC9/GR cells treated with the control (DMSO) or 200uM Zileuton.

    Zileuton purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2019 Oct. 

    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 MCE. Usage Cited in: Oxid Med Cell Longev. 2019 Oct. 

    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).
    • Biological Activity

    • Protocol

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    • References

    • Customer Review

    Description

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

    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].

    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].

    Clinical Trial
    Molecular Weight

    236.29

    Formula

    C₁₁H₁₂N₂O₂S

    CAS No.

    111406-87-2

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (423.21 mM)

    *"≥" means soluble, but saturation unknown.

    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
    10 mM 0.4232 mL 2.1160 mL 4.2321 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    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
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    Keywords:

    ZileutonA 64077Abbott 64077A64077A-64077Abbott64077Abbott-640775-Lipoxygenase5-LOX5-LOInhibitorinhibitorinhibit

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    Product name:
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    Cat. No.:
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