Omaveloxolone (RTA-408)

Catalog No.S7672 Batch:S767202

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Technical Data

Formula

C33H44F2N2O3
Molecular Weight 554.71 CAS No. 1474034-05-3
Solubility (25°C)* In vitro DMSO 100 mg/mL (180.27 mM)
Ethanol 3 mg/mL (5.4 mM)
Water Insoluble
In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Omaveloxolone (RTA-408) is a synthetic triterpenoid that activates the cytoprotective transcription factor Nrf2 and inhibits NF-κB signaling. Phase 2.
Targets
NF-κB Nrf2
In vitro 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 tumour 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 tumour cells.
In Vivo In 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.

Protocol (from reference)

Cell Assay:[1]
  • Cell Lines

    A375, NCI-H460, A2058, MDA-Mb-231, HCT116, 786-0, A549, and PANC-1 cells

  • Concentrations

    ~1 μM

  • Incubation Time

    72 hours

  • Method

    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
Animal Study:[2]
  • Animal Models

    Mice with radiation-induced dermatitis

  • Dosages

    1% in 100 μL vehicle (w/v)

  • Administration

    Topical application

References

  • https://pubmed.ncbi.nlm.nih.gov/25897966/
  • https://pubmed.ncbi.nlm.nih.gov/24720753/
  • https://pubmed.ncbi.nlm.nih.gov/24362512/
  • https://pubmed.ncbi.nlm.nih.gov/25738896/

Sellecks Omaveloxolone (RTA-408) Has Been Cited by 11 Publications

Disruption of the KLHL37-N-Myc complex restores N-Myc degradation and arrests neuroblastoma growth in mouse models [ J Clin Invest, 2025, 135(14)e176655] PubMed: 40493396
Bidirectional regulation of KEAP1 BTB domain-based sensor activity [ Redox Biol, 2025, 87:103885] PubMed: 41092551
Computational drug repurposing in Parkinson's disease: Omaveloxolone and cyproheptadine as promising therapeutic candidates [ Front Pharmacol, 2025, 16:1539032] PubMed: 40264664
Inhibiting the RNA helicase DDX3X in Burkitt lymphoma induces oxydative stress and impedes tumor progression in xenografts [ Front Cell Dev Biol, 2025, 13:1642006] PubMed: 40772229
Synthetic oleanane triterpenoids suppress MYB oncogene activity and sensitize T-cell acute lymphoblastic leukemia cells to chemotherapy [ Front Oncol, 2023, 13:1126354] PubMed: 37077825
Activadores del factor de transcripción NRF2 (factor nuclear eritroide 2) en el tratamiento de la Enfermedad Pulmonar Obstructiva Crónica [ University of Valencia, 2023, ] PubMed: None
Neonatal ketone body elevation regulates postnatal heart development by promoting cardiomyocyte mitochondrial maturation and metabolic reprogramming [ Cell Discov, 2022, 8(1):106] PubMed: 36220812
RTA-408 protects against propofol-induced cognitive impairment in neonatal mice via the activation of Nrf2 and the inhibition of NF-κB p65 nuclear translocation [ Brain Behav, 2021, 11(1):e01918] PubMed: 33295701
A Human Organoid Model of Aggressive Hepatoblastoma for Disease Modeling and Drug Testing [ Cancers (Basel), 2020, 12(9)E2668] PubMed: 32962010
Inhibition of Nrf2 might enhance the anti-tumor effect of temozolomide in glioma cells via inhibition of Ras/Raf/MEK signaling pathway. [ Int J Neurosci, 2020, 7:1-16] PubMed: 32378973

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.