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    Omaveloxolone (RTA-408)
    Omaveloxolone (RTA-408)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1891
    CAS #: 1474034-05-3Purity ≥98%

    Description: Omaveloxolone (formerly known as RTA-408; RTA408), an antioxidant inflammation modulator (AIM), is a 2nd generation member of the synthetic triterpenoid that can activate Nrf2 (a cytoprotective transcription factor) and inhibit NF-κB signaling. As an Nrf2 activator, Omaveloxolone improves mitochondrial function, restores redox balance, and reduces inflammation in models of FA. Upon administration, RTA 408 activates the cytoprotective transcription factor Nrf2. In turn, Nrf2 translocates to the nucleus, dimerizes with a small Maf protein (sMaf), and binds to the antioxidant response element (ARE). This induces the expression of a number of cytoprotective genes, including NAD(P)H quinone oxidoreductase 1 (NQO1), sulfiredoxin 1 (Srxn1) etc.

    References: PLoS One. 2015 Apr 21;10(4):e0122942; Radiat Res. 2014 May;181(5):512-20. 

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    Molecular Weight (MW)554.71 
    FormulaC33H44F2N2O3 
    CAS No.1474034-05-3 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (180.3 mM) 
    Water: <1 mg/mL
    Ethanol: 20 mg/mL (36.1 mM) 
    Solubility (In vivo)10%DMSO+90% Corn oil: 30mg/mL 
    SynonymsRTA 408; RTA408; RTA-408


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    In Vitro

    In vitro activity: RTA 408 potently increases expression of Nrf2 target genes and reverses IFNγ-mediated suppression of Gclc expression in RAW 264.7 cells. In a panel of eight human tumor cell lines, RTA 408 inhibits growth with an average GI50 value of 260 nM and induces apoptosis. RTA 408 also inhibits NF-κB and activates JNK in tumor cells.


    Cell Assay: For growth inhibition assays, cells are plated in duplicate 96-well culture dishes at 3 x 103 cells per well. The following day, one plate is treated with RTA 408 and the other is immediately processed for the sulforhodamine B (SRB) assay (time 0). Cells in the RTA 408-treated plate are processed for the SRB assay 72 hours after the start of treatment. Percentage of growth relative to vehicle-treated cells is calculated using: [(Ti-Tz)/(C-Tz)] x 100 where (Tz) is the absorbance value at time zero, (C) is absorbance value from vehicle treated wells after 72 hours, and (Ti) is the absorbance value from wells treated with the drug. Dose-response curves are plotted in GraphPad Prism and GI50 values are calculated.

    In VivoIn mice with radiation-induced dermatitis, 1.0% RTA 408 markedly reduces epidermal and collagen thickening, prevents dermal necrosis and completely alleviates skin ulcers. In rat skin, RTA 408 activates Nrf2 and induces cytoprotective genes. RTA 408 also mitigates hematopoietic acute radiation syndrome in mice. 
    Animal modelMice with radiation-induced dermatitis 
    Formulation & DosageDissolved in sesame oil; 1% in 100 μL vehicle (w/v); Topical application 
    References

    PLoS One. 2015 Apr 21;10(4):e0122942; Radiat Res. 2014 May;181(5):512-20; Arch Dermatol Res. 2014 Jul;306(5):447-54.  


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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