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Omaveloxolone

Catalog No. T6919   CAS 1474034-05-3
Synonyms: RTA-408

Omaveloxolone (RTA-408) (RTA-408) is a synthetic triterpenoid that activates the cytoprotective transcription factor Nrf2 and inhibits NF-κB signaling. Phase 2.

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Omaveloxolone Chemical Structure
Omaveloxolone, CAS 1474034-05-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 38.00
2 mg In stock $ 54.00
5 mg In stock $ 89.00
10 mg In stock $ 122.00
25 mg In stock $ 222.00
50 mg In stock $ 372.00
100 mg In stock $ 538.00
500 mg In stock $ 1,150.00
1 mL * 10 mM (in DMSO) In stock $ 109.00
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Purity: 98.7%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Omaveloxolone (RTA-408) (RTA-408) is a synthetic triterpenoid that activates the cytoprotective transcription factor Nrf2 and inhibits NF-κB signaling. Phase 2.
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 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. [1]
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. [2] In rat skin, RTA 408 activates Nrf2 and induces cytoprotective genes. [3] RTA 408 also mitigates hematopoietic acute radiation syndrome in mice. [4]
Cell Research 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(Only for Reference)
Synonyms RTA-408
Molecular Weight 554.71
Formula C33H44F2N2O3
CAS No. 1474034-05-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 16 mg/mL (28.8 mM)

DMSO: 93 mg/mL (167.7 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Probst BL, et al. PLoS One. 2015, 10(4), e20122942. 2. Reisman SA, et al. Radiat Res. 2014, 181(5), 512-520. 3. Reisman SA, et al. Arch Dermatol Res. 2014, 306(5), 447-454. 4. Goldman DC, et al. Radiat Res. 2015, 183(3), 338-344.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Inhibitor Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Clinical Compound Library PPI Inhibitor Library Anti-Lung Cancer Compound Library Anti-Cancer Compound Library Anti-Obesity Compound Library

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Keywords

Omaveloxolone 1474034-05-3 Apoptosis Immunology/Inflammation Others Nrf2 STING Inhibitor ERIS inhibit Stimulator of Interferon Genes RTA408 TMEM173 RTA-408 RTA 408 MITA Keap1-Nrf2 MPYS inhibitor

 

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