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Bardoxolone methyl (Synonyms: NSC 713200; RTA 402; CDDO Methyl ester)

Cat. No.: HY-13324 Purity: 98.35%
Handling Instructions

Bardoxolone (methyl) is a potent activator of the nuclear factor erythroid 2-related factor 2 (Nrf2), and uesd for antioxidative and anti-inflammatory treatment.

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

Bardoxolone methyl Chemical Structure

Bardoxolone methyl Chemical Structure

CAS No. : 218600-53-4

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
10 mg USD 50 In-stock
Estimated Time of Arrival: December 31
50 mg USD 100 In-stock
Estimated Time of Arrival: December 31
100 mg USD 150 In-stock
Estimated Time of Arrival: December 31
200 mg USD 250 In-stock
Estimated Time of Arrival: December 31
500 mg USD 540 In-stock
Estimated Time of Arrival: December 31
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Other Forms of Bardoxolone methyl:

    Bardoxolone methyl purchased from MCE. Usage Cited in: Toxicol Lett. 2016 Jul 29;259:52-59.

    MATE1/SCL47A1 efflux transporter expression in hPTCs. Protein (n=3) expression is assessed after administration of Cisplatin and pre- or delayedexposure to CDDO-Me after 12 h. GAPDH is used as a housekeeping gene. β-actin is used as a loading control.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Bardoxolone (methyl) is a potent activator of the nuclear factor erythroid 2-related factor 2 (Nrf2), and uesd for antioxidative and anti-inflammatory treatment.

    In Vivo

    Bardoxolone Methyl (30 mg/kg, p.o.) decreases renal expression of megalin but not cubilin, increases creatinine clearance and urinary albumin-to-creatinine ratios, and induces Nrf2 cytoprotective targets in cynomolgus monkeys[1]. Bardoxolone Methyl could induce overall favorable effects on the heart via its improvement in eGFR in both animal models and clinical trials[2].

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 49 mg/mL (96.90 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9775 mL 9.8875 mL 19.7750 mL
    5 mM 0.3955 mL 1.9775 mL 3.9550 mL
    10 mM 0.1977 mL 0.9887 mL 1.9775 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [1]

    Kidney tissue from the 28-day monkey study is snap-frozen in liquid nitrogen, and stored at -80°C until analysis. Kidney tissue is homogenized at 250 mg tissue/mL ice cold PBS (pH 7.2), containing 2 mM ethylenediaminetetraacetic acid (EDTA). Homogenates are then centrifuged at 10,000 x g for 10 minutes at 4°C. The supernatants are collected and stored at -80°C until analysis. Protein concentrations of tissue homogenates are determined using the Bicinchoninic Acid (BCA) Protein Assay Kit from Pierce Biotechnology. NQO1 enzyme activity is determined by quantifying the rate of reduction of 2,6-dichlorophenol-indophenol (DCPIP). Gsr enzyme activity is determined using a commercially available kit. All enzyme activities are normalized to protein and presented as fold vehicle control.

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

    Animal Administration
    [1]

    Two separate in-life studies are conducted in cynomolgus monkeys. In one study, cynomolgus monkeys (n=9/gender/dose group) are administered amorphous bardoxolone methyl by oral gavage, using sesame oil as the vehicle, at 5, 30, and 300 mg/kg once daily for 12 months in a GLP environment. Observations for morbidity, mortality, injury, and the availability of food and water are conducted twice daily for all animals. Clinical observations and body weights are conducted and recorded weekly. Weight data are analyzed by calculating the area under the weight versus time curve using the linear trapezoidal method. Blood samples for clinical chemistry evaluations are collected from all animals pretest and from all animals prior to interim (6-month) and terminal (12-month) necropsies. An additional group of monkeys for each dose group are allowed to recover for 4 weeks.

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

    References
    Molecular Weight

    505.69

    Formula

    C₃₂H₄₃NO₄

    CAS No.

    218600-53-4

    SMILES

    O=C1C(C#N)=C[[email protected]@]2(C)[[email protected]](CC[[email protected]]([[email protected]@]3(C)[[email protected]@]4([H])[[email protected]@]5([H])[[email protected]@](CCC(C)(C)C5)(C(OC)=O)CC3)(C)C2=CC4=O)([H])C1(C)C

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 98.35%

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    Product Name:
    Bardoxolone methyl
    Cat. No.:
    HY-13324
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    Bardoxolone methyl

    Cat. No.: HY-13324