Art. -Nr.: HY-12212

Omaveloxolone

(Synonyms: RTA 408)

26 Cited Publications

Kundenbewertung

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.

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Reinheit: 99.29%
CAS. Nr.: 1474034-05-3
Formel: C₃₃H₄₄F₂N₂O₃
Molecular Weight:554.71

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Omaveloxolone Chemical Structure

CAS. Nr.: 1474034-05-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (26)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Nrf2^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HT-29	EC₅₀	1.41 μM Compound: 12; RTA-408	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	[PMID: 33248849]
L929	EC₅₀	5.25 μM Compound: 12; RTA-408	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	[PMID: 33248849]

In Vitro

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.

In Vivo

To determine whether Omaveloxolone (RTA-408) is an effective mitigator of hematopoietic acute radiation syndrome after bone marrow-lethal doses of total-body irradiation (TBI), mice are administered 3 daily injections of 17.5 mg/kg Omaveloxolone beginning 24 h after TBI. Teatment with Omaveloxolone results in the 35 day survival of 100% of 7 Gy (LD_40/35) TBI mice (P<0.05) and 60% of 7.5 Gy (LD_100/13) TBI mice (P<0.0001)^[2].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1474034-05-3
Appearance Solid
Molecular Weight 554.71
Formel C₃₃H₄₄F₂N₂O₃
Color White to off-white
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
Synonyms

RTA 408
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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.
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
Osteoarthritis Cartilage

Age and oxidative stress regulate Nrf2 homeostasis in human articular chondrocytes. [Abstract]

2023 Sep;31(9):1214-1223. PMID: 37160250
Antioxidants (Basel)

The Xanthine Oxidase Inhibitor Febuxostat Suppresses Adipogenesis and Activates Nrf2. [Abstract]

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
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
Eur J Med Chem

Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors. [Abstract]

2021 Feb 15;212:113030. PMID: 33248849
Inflamm Res

KIAA1429 Silencing ameliorates osteosarcoma progression through promoting ferroptosis via Nrf2/NQO1 axis. [Abstract]

2025 Aug 22;74(1):111. PMID: 40844619
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
Int Immunopharmacol

RTA408 alleviates lipopolysaccharide-induced acute lung injury via inhibiting Bach1-mediated ferroptosis. [Abstract]

2024 Sep 27;142(Pt B):113250. PMID: 39340988
Int J Mol Sci

Monitoring Nrf2/ARE Pathway Activity with a New Zebrafish Reporter System. [Abstract]

2023 Apr 6;24(7):6804. PMID: 37047777
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
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
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
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
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
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
Mol Immunol

Dehydroepiandrosterone attenuates LPS-induced inflammatory responses via activation of Nrf2 in RAW264.7 macrophages. [Abstract]

2021 Mar:131:97-111. PMID: 33461765
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

RTA-408 induces JNK-dependent apoptosis and autophagy in breast cancer cells. [Abstract]

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.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8027 mL

9.0137 mL

18.0274 mL

5 mM

0.3605 mL

1.8027 mL

3.6055 mL

10 mM

0.1803 mL

0.9014 mL

1.8027 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.51 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Cell Assay^[1]

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.

Animal Administration^[2]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

[2]. Peng Han, et al. RTA-408 Protects Kidney from Ischemia-Reperfusion Injury in Mice via Activating Nrf2 and Downstream GSH Biosynthesis Gene. Oxid Med Cell Longev. 24 December 2017.

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Omaveloxolone

26 Cited Publications

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Omaveloxolone

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Publications Citing Use of MedChemExpress (MCE) Omaveloxolone

Biologische Aktivität

Chemical Information

Publications (26)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Omaveloxolone Related Classifications

HY-12212 Related Classifications