Omaveloxolone
Based on 26 publication(s) in Google Scholar
Omaveloxolone (RTA 408) is an antioxidant inflammation modulator (AIM), which activates Nrf2 and suppresses nitric oxide (NO). Omaveloxolone attenuates osteoclastogenesis by inhibiting STING dependent NF-κb signaling.
For research use only. We do not sell to patients.
- Purity: 99.29%
- CAS No.: 1474034-05-3
- Formula: C33H44F2N2O3
- Molecular Weight:554.71
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
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Publications Citing Use of MedChemExpress (MCE) Omaveloxolone
More- Cell Metab. 2021 Jun 1;33(6):1205-1220.e5. [Abstract]
- Redox Biol. 2020 Jan;28:101309. [Abstract]
- Osteoarthritis Cartilage. 2023 Sep;31(9):1214-1223. [Abstract]
- Free Radic Biol Med. 2024 Aug 1:220:15-27. [Abstract]
- Free Radic Biol Med. 2024 Feb 20:212:415-432. [Abstract]
- Cell Death Discov. 2025 Dec 23;11(1):563. [Abstract]
- Antioxidants (Basel). 2023 Jan 5;12(1):133. [Abstract]
- Antioxidants (Basel). 2021 Sep 15;10(9):1466. [Abstract]
- Eur J Med Chem. 2021 Feb 15;212:113030. [Abstract]
- Neurobiol Dis. 2023 Aug:184:106210. [Abstract]
- Inflamm Res. 2025 Aug 22;74(1):111. [Abstract]
- Inflammation. 2019 Oct;42(5):1843-1856. [Abstract]
- Int J Mol Sci. 2023 Apr 6;24(7):6804. [Abstract]
- Int Immunopharmacol. 2024 Sep 27;142(Pt B):113250. [Abstract]
- Neuropharmacology. 2026 Aug 1:293:110940. [Abstract]
- Neuropharmacology. 2025 Jan 15:110312. [Abstract]
- Viruses. 2026 May 9;18(5):548. [Abstract]
- Viruses. 2023 Feb 28;15(3):655. [Abstract]
- Viruses. 2022 Dec 15;14(12):2799. [Abstract]
- J Immunol. 2025 Jun 16:vkaf117. [Abstract]
- Mol Immunol. 2021 Mar:131:97-111. [Abstract]
- Adv Redox Res. 2026 Mar:18:100158. [Abstract]
- PLoS One. 2020 Oct 5;15(10):e0240122. [Abstract]
- Oncol Lett. 2026 Jun 11;32(2):337. [Abstract]
- Oxid Med Cell Longev. 2022 Mar 11:2022:4564471. [Abstract]
- Oxid Med Cell Longev. 2017:2017:7612182. [Abstract]
Customer Validation & Images
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IF
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Biological Activity
Nrf2[1]
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Cell Line
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Type | Value | Description | References |
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| HT-29 | EC50 |
1.41 μM
Compound: 12; RTA-408
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Anti-necroptotic activity in human HT-29 cells assessed as inhibition of TNFalpha/SM-164/Z-VAD-fmk (TSZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay
Anti-necroptotic activity in human HT-29 cells assessed as inhibition of TNFalpha/SM-164/Z-VAD-fmk (TSZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay
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[PMID: 33248849] |
| L929 | EC50 |
5.25 μM
Compound: 12; RTA-408
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Anti-necroptotic activity in mouse L929 cells assessed as inhibition of TNFalpha/Z-VAD-fmk (TZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay
Anti-necroptotic activity in mouse L929 cells assessed as inhibition of TNFalpha/Z-VAD-fmk (TZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay
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[PMID: 33248849] |
To evaluate the anti-inflammatory activity of Omaveloxolone (RTA 408), RAW 264.7 mouse macrophage cells are treated with Omaveloxolone for two hours and then IFNγ is added to stimulate NO production and release into the media. Omaveloxolone dose-dependently reduces NO concentrations in the media with an IC50 value of 4.4±1.8 nM. The potency of Omaveloxolone in this assay is similar to that of Bardoxolone methyl, which has an IC50 value of 1.9±0.8 nM. Nrf2 activation is required for AIM-mediated NO suppression. A decrease in nitric oxide synthase 2 (Nos2) protein levels is observed in bardoxolone methyl-treated RAW 264.7 cells, which is attenuated when Nrf2 mRNA levels are reduced by siRNA. To evaluate the anticancer activity of Omaveloxolone, a panel of eight human cell lines derived from tumors of different origin are treated with Omaveloxolone and measured cell growth 72 hours later using the sulforhodamine B (SRB) assay. Omaveloxolone inhibits the growth of all tumor lines with an average GI50 value of 260±74 nM. To determine whether Omaveloxolone induces apoptosis, the panel of tumor cells are treated with Omaveloxolone and the caspase substrate, DEVD-AFC, for 24 hours. Omaveloxolone dose-dependently increases DEVD-AFC cleavage, indicating that Omaveloxolone treatment triggers caspase activation in cancer cells. Caspase-3 and caspase-9 cleavage is also observed by western blot at the same concentrations of Omaveloxolone that increases DEVD-AFC cleavage[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1474034-05-3
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Appearance Solid
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Molecular Weight 554.71
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Formula C33H44F2N2O3
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Color White to off-white
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SMILES
O=C1C(C#N)=C[C@@]2(C)[C@](CC[C@]([C@@]3(C)[C@@]4([H])[C@@]5([H])[C@@](CCC(C)(C)C5)(NC(C(F)(F)C)=O)CC3)(C)C2=CC4=O)([H])C1(C)C
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Synonyms
RTA 408
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (26)
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Journal Impact Factor
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Most Recent
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Cell Metab
Metabolic flexibility determines human NK cell functional fate in the tumor microenvironment. [Abstract]2021 Jun 1;33(6):1205-1220.e5. PMID: 33852875 -
Redox Biol
The Nrf2 activator RTA-408 attenuates osteoclastogenesis by inhibiting STING dependent NF-κb signaling. [Abstract]2020 Jan;28:101309. PMID: 31487581
Omaveloxolone purchased from MedChemExpress. Usage Cited in: Redox Biol. 2020 Jan;28:101309. [Abstract]
F-Actin ring formation assays are carried to detect the effect of RTA-408 on the generation of mature osteoclasts. The actin rings were detected using phalloidin with fluorescence microscopy after RTA-408 treatment (20 nM).
Omaveloxolone purchased from MedChemExpress. Usage Cited in: Redox Biol. 2020 Jan;28:101309. [Abstract]
The protein level of STING was analyzed by western blotting on day 2 and 4 of osteoclastogenesis in the presence of RTA-408.
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Osteoarthritis Cartilage
2023 Sep;31(9):1214-1223. PMID: 37160250 -
Free Radic Biol Med
The NRF2 activator RTA-408 ameliorates chronic alcohol exposure-induced cognitive impairment and NLRP3 inflammasome activation by modulating impaired mitophagy initiation. [Abstract]2024 Aug 1:220:15-27. PMID: 38679301 -
Free Radic Biol Med
Reduced Zn2+ promotes retinal ganglion cells survival and optic nerve regeneration after injury through inhibiting autophagy mediated by ROS/Nrf2. [Abstract]2024 Feb 20:212:415-432. PMID: 38134974 -
Cell Death Discov
Ferroptosis is a novel pathogenic mechanism of FDXR-related disease via disruption of the NRF2 pathway. [Abstract]2025 Dec 23;11(1):563. PMID: 41436440 -
Antioxidants (Basel)
2023 Jan 5;12(1):133. PMID: 36670994 -
Antioxidants (Basel)
The Effects of Two Nrf2 Activators, Bardoxolone Methyl and Omaveloxolone, on Retinal Ganglion Cell Survival during Ischemic Optic Neuropathy. [Abstract]2021 Sep 15;10(9):1466. PMID: 34573098 -
Eur J Med Chem
2021 Feb 15;212:113030. PMID: 33248849 -
Neurobiol Dis
NRF2 activation suppresses motor neuron ferroptosis induced by the SOD1G93A mutation and exerts neuroprotection in amyotrophic lateral sclerosis. [Abstract]2023 Aug:184:106210. PMID: 37352984 -
Inflamm Res
KIAA1429 Silencing ameliorates osteosarcoma progression through promoting ferroptosis via Nrf2/NQO1 axis. [Abstract]2025 Aug 22;74(1):111. PMID: 40844619 -
Inflammation
Nrf2 Activator RTA-408 Protects Against Ozone-Induced Acute Asthma Exacerbation by Suppressing ROS and γδT17 Cells. [Abstract]2019 Oct;42(5):1843-1856. PMID: 31256292 -
Int J Mol Sci
2023 Apr 6;24(7):6804. PMID: 37047777 -
Int Immunopharmacol
RTA408 alleviates lipopolysaccharide-induced acute lung injury via inhibiting Bach1-mediated ferroptosis. [Abstract]2024 Sep 27;142(Pt B):113250. PMID: 39340988 -
Neuropharmacology
Targeting ME1 rescues redox-metabolic coordination in ALS: A core effector of NRF2-directed therapy. [Abstract]2026 Aug 1:293:110940. PMID: 41903869 -
Neuropharmacology
Swietenolide inhibits the TXNIP/NLRP3 pathways via Nrf2 activation to ameliorate cognitive dysfunction in diabetic mice. [Abstract]2025 Jan 15:110312. PMID: 39824302 -
Viruses
Application of a Blood-Brain Barrier Organ-on-a-Chip Model for Assessment of Countermeasure Efficiency Against Eastern Equine Encephalitis Virus. [Abstract]2026 May 9;18(5):548. PMID: 42198751 -
Viruses
Inhibitors of the Ubiquitin-Mediated Signaling Pathway Exhibit Broad-Spectrum Antiviral Activities against New World Alphaviruses. [Abstract]2023 Feb 28;15(3):655. PMID: 36992362 -
Viruses
Application of a Human Blood Brain Barrier Organ-on-a-Chip Model to Evaluate Small Molecule Effectiveness against Venezuelan Equine Encephalitis Virus. [Abstract]2022 Dec 15;14(12):2799. PMID: 36560802 -
J Immunol
Therapeutic potential of NRF2 activating drug RTA-408 in suppressing T cell effector responses and inflammatory bowel disease. [Abstract]2025 Jun 16:vkaf117. PMID: 40570091 -
Mol Immunol
Dehydroepiandrosterone attenuates LPS-induced inflammatory responses via activation of Nrf2 in RAW264.7 macrophages. [Abstract]2021 Mar:131:97-111. PMID: 33461765 -
Adv Redox Res
Inhibition of smooth muscle phenotypic modulation by bardoxolone methyl, omaveloxolone, and cinnamaldehyde is Nrf-2 dependent. [Abstract]2026 Mar:18:100158. PMID: 41891110 -
PLoS One
Mechanisms and therapeutic implications of RTA 408, an activator of Nrf2, in subarachnoid hemorrhage-induced delayed cerebral vasospasm and secondary brain injury. [Abstract]2020 Oct 5;15(10):e0240122. PMID: 33017422 -
Oncol Lett
2026 Jun 11;32(2):337. PMID: 42325926 -
Oxid Med Cell Longev
The Novel Nrf2 Activator Omaveloxolone Regulates Microglia Phenotype and Ameliorates Secondary Brain Injury after Intracerebral Hemorrhage in Mice. [Abstract]2022 Mar 11:2022:4564471. PMID: 35308167 -
Oxid Med Cell Longev
RTA-408 Protects Kidney from Ischemia-Reperfusion Injury in Mice via Activating Nrf2 and Downstream GSH Biosynthesis Gene. [Abstract]2017:2017:7612182. PMID: 29435098
Omaveloxolone purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2017:2017:7612182. [Abstract]
Nuclear translocation of Nrf2 by RTA-408 is measured by immunohistochemistry staining.
Solvent & Solubility
DMSO : 100 mg/mL (180.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
MEFs, PANC-1, A549, A375, A549/NF-κB-Luc and HeLa/NF-κB-Luc cells are cultured in Gibco high glucose DMEM with 10% FBS. G-361 cells are cultured in McCoy’s 5A medium with 10% FBS. All other cell lines are cultured in RPMI 1640 medium with 10% FBS. For growth inhibition assays, cells are plated in duplicate 96-well culture dishes at 3×103 cells per well. The following day, one plate is treated with Omaveloxolone (200, 400, 600, 800 and 1000 nM) and the other is immediately processed for the sulforhodamine B (SRB) assay (time 0). Cells in the Omaveloxolone-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. Dose-response curves are plotted in GraphPad Prism and GI50 values are calculated. For cell counting experiments, MEFs are plated in 6-well culture dishes at 5×104 cells per well and treated with Omaveloxolone the following day. Following treatment, cells are counted using a Vi-CELL XR cell analyzer. For clonogenic assays, wild-type (1×103 cells per well) and Keap1-/- (0.5×103 cells per well) MEFs are seeded in 6-well dishes. Six hours later, MEFs are treated with Omaveloxolone. After seven days, colonies are fixed with a 1:7 solution of acetic acid:MeOH and stained with 0.5% crystal violet in MeOH. Colonies consisting of ≥50 cells are counted[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
For radiation survival experiments, wild-type C57Bl/6 CD45.2 mice (6-8 weeks old) are used. Congenic wild-type C57Bl/6 CD45.1 and C57Bl/6 CD45.1/CD45.2 hybrid host mice are used as recipients in transplantation experiments. Omaveloxolone stock solutions for vehicle control (DMSO) are prepared within 1 h before injection. Omaveloxolone (17.5 mg/kg) or DMSO is administered intraperitoneally at 24, 48 and 72 h after irradiation. Whole-body irradiation (7-8 Gy) is performed using a 250-kVp X-ray machine with 50 cm source-to-skin distance and a 2 mm copper filter. The dose rate is approximately 1.4 Gy/min.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Probst BL, et al. RTA 408, A Novel Synthetic Triterpenoid with Broad Anticancer and Anti-Inflammatory Activity. PLoS One. 2015 Apr 21;10(4):e0122942. [Content Brief]
[3]. Goldman DC, et al. The triterpenoid RTA 408 is a robust mitigator of hematopoietic acute radiation syndrome in mice. Radiat Res. 2015 Mar;183(3):338-44 [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8027 mL | 9.0137 mL | 18.0274 mL | 45.0686 mL |
| 5 mM | 0.3605 mL | 1.8027 mL | 3.6055 mL | 9.0137 mL | |
| 10 mM | 0.1803 mL | 0.9014 mL | 1.8027 mL | 4.5069 mL | |
| 15 mM | 0.1202 mL | 0.6009 mL | 1.2018 mL | 3.0046 mL | |
| 20 mM | 0.0901 mL | 0.4507 mL | 0.9014 mL | 2.2534 mL | |
| 25 mM | 0.0721 mL | 0.3605 mL | 0.7211 mL | 1.8027 mL | |
| 30 mM | 0.0601 mL | 0.3005 mL | 0.6009 mL | 1.5023 mL | |
| 40 mM | 0.0451 mL | 0.2253 mL | 0.4507 mL | 1.1267 mL | |
| 50 mM | 0.0361 mL | 0.1803 mL | 0.3605 mL | 0.9014 mL | |
| 60 mM | 0.0300 mL | 0.1502 mL | 0.3005 mL | 0.7511 mL | |
| 80 mM | 0.0225 mL | 0.1127 mL | 0.2253 mL | 0.5634 mL | |
| 100 mM | 0.0180 mL | 0.0901 mL | 0.1803 mL | 0.4507 mL |
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