1. Metabolic Enzyme/Protease Apoptosis
  2. Mitochondrial Metabolism Apoptosis
  3. Idebenone

Idebenone, a well-appreciated mitochondrial protectant, exhibits protective efficacy against neurotoxicity and can be used for the research of Alzheimer's disease, Huntington's disease. Idebenone (oxidised form) has a dose-dependent inhibitory effect on the enzymatic metabolism of arachidonic acid in astroglial homogenates (IC50=16.65 μM). Idebenone, a coenzyme Q10 analog and an antioxidant, induces apoptotic cell death in the human dopaminergic neuroblastoma SHSY-5Y cells. Idebenone quickly crosses the blood-brain barrier.

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Idebenone Chemical Structure

Idebenone Chemical Structure

CAS No. : 58186-27-9

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10 mM * 1 mL in DMSO
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Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Idebenone purchased from MedChemExpress. Usage Cited in: Oncotarget. 2018 Jan 30;9(15):12137-12153.  [Abstract]

    Retinal protection of Rasagiline combined with Idebenone against retinal ischemia-reperfusion (RIR) injury. Western blot analysis for the expression level of brain-derived neurotrophic factor (BDNF) in the whole IR-injured retinas.
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    • Purity & Documentation

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    • Customer Review

    Description

    Idebenone, a well-appreciated mitochondrial protectant, exhibits protective efficacy against neurotoxicity and can be used for the research of Alzheimer's disease, Huntington's disease. Idebenone (oxidised form) has a dose-dependent inhibitory effect on the enzymatic metabolism of arachidonic acid in astroglial homogenates (IC50=16.65 μM)[1]. Idebenone, a coenzyme Q10 analog and an antioxidant, induces apoptotic cell death in the human dopaminergic neuroblastoma SHSY-5Y cells[2]. Idebenone quickly crosses the blood-brain barrier.

    In Vitro

    Idebenone, a compound with protective efficacy against neurotoxicity both in in vitro and in in vivo models, exists in two different oxidative states: the ubiquinol-derivative (reduced idebenone) and the ubiquinone-derivative (oxidised idebenone)[1].
    ? Idebenone (oxidised form) preferentially inhibits cyclooxygenase vs. lipoxygenase metabolism (IC50 ratio lipoxygenase/cyclooxygenase: 3.22)[1].
    ? Idebenone (oxidised form) behaves similarly as indomethacin and piroxicam—two typical anti-inflammatory agents[1].
    ? Idebenone (oxidised form) inhibits total arachidonic acid metabolism, cyclooxygenase metabolism, lipoxygenase metabolism, lipoxygenase/cyclooxygenase with IC50s of 16.65±3.48, 14.44±2.99, 46.51±7.20, and 3.22 μM[1].
    ? Idebenone (1-10 μM; for 24-72 h) has no effect on the cell viability of SHSY-5Y cells[2].
    ? Idebenone (25 μM or higher concentrations; for 24-72 h) shows significant reduction in cell viability of SHSY-5Y cells[2]. ? Idebenone (30 μM) induces up-regulation of BAX expression and the caspase-3 activity[2].

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

    Cell Viability Assay[2]

    Cell Line: The human dopaminergic neuroblastma cell line, SHSY-5Y cells
    Concentration: 1, 3, 10, 15, 25, 30, and 90 μM
    Incubation Time: 24, 48, and 72 hours
    Result: Had no apparent detrimental effects on cell viability as indicated by the absence of trypan blue-positive staining in the cells at concentrations of 1, 3, 10 μM.
    Exhibited some degree of trypan blue-positive staining at 15 μM. Showed extensive trypan blue-positive staining at 25 μM and 30 μM.

    RT-PCR[2]

    Cell Line: SHSY-5Y cells
    Concentration: 10 μM, 30 μM
    Incubation Time: 72 hours
    Result: The total RNA of BAX from SHSY-5Y cells exposed to 10 μM was not different from that of the untreated control cells.
    The BAX expression in SHSY-5Y cells exposed to 30 μM was significantly up-regulated when compared with the untreated control cells and cells exposed to 10 μM.
    In Vivo

    Idebenone (oxidised form) is a compound with protective efficacy against cerebrovascular disorders in vivo, including cerebral ischemia and hypertension-induced vascular lesions[1].

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

    Clinical Trial
    Molecular Weight

    338.44

    Formula

    C19H30O5

    CAS No.
    Appearance

    Solid

    Color

    Yellow to orange

    SMILES

    O=C1C(CCCCCCCCCCO)=C(C)C(C(OC)=C1OC)=O

    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 (295.47 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.9547 mL 14.7737 mL 29.5473 mL
    5 mM 0.5909 mL 2.9547 mL 5.9095 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.

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

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    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 (7.39 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      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 (7.39 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      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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    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

    Purity: 99.36%

    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 2.9547 mL 14.7737 mL 29.5473 mL 73.8683 mL
    5 mM 0.5909 mL 2.9547 mL 5.9095 mL 14.7737 mL
    10 mM 0.2955 mL 1.4774 mL 2.9547 mL 7.3868 mL
    15 mM 0.1970 mL 0.9849 mL 1.9698 mL 4.9246 mL
    20 mM 0.1477 mL 0.7387 mL 1.4774 mL 3.6934 mL
    25 mM 0.1182 mL 0.5909 mL 1.1819 mL 2.9547 mL
    30 mM 0.0985 mL 0.4925 mL 0.9849 mL 2.4623 mL
    40 mM 0.0739 mL 0.3693 mL 0.7387 mL 1.8467 mL
    50 mM 0.0591 mL 0.2955 mL 0.5909 mL 1.4774 mL
    60 mM 0.0492 mL 0.2462 mL 0.4925 mL 1.2311 mL
    80 mM 0.0369 mL 0.1847 mL 0.3693 mL 0.9234 mL
    100 mM 0.0295 mL 0.1477 mL 0.2955 mL 0.7387 mL
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      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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