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Omaveloxolone

(Synonyms: RTA-408) Copy Product Info
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Synonyms: RTA-408

Catalog No. T6919 Copy Product Info
Purity: 99.92%
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Omaveloxolone (RTA-408) is an oral, potent, and selective activator of the nuclear factor erythropoietin-related factor 2 (Nrf2) pathway, as well as a low-potency PPARγ agonist. Omaveloxolone inhibits osteoclast formation by suppressing the STING-dependent NF-κB signaling pathway. Omaveloxolone is being investigated for use in ALS, multiple sclerosis, non-alcoholic steatohepatitis, neurodegenerative diseases, and oncology research.
Omaveloxolone
Cas No. 1474034-05-3
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Pack SizePriceUSA StockGlobal StockQuantity
1 mg$38-In Stock
2 mg$54-In Stock
5 mg$89-In Stock
10 mg$122-In Stock
25 mg$222-In Stock
50 mg$372-In Stock
100 mg$538-In Stock
500 mg$1,150-In Stock
1 mL x 10 mM (in DMSO)$109-In Stock
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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Purity:99.92%
Color:White
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Product Introduction

Bioactivity
Description
Omaveloxolone (RTA-408) is an oral, potent, and selective activator of the nuclear factor erythropoietin-related factor 2 (Nrf2) pathway, as well as a low-potency PPARγ agonist. Omaveloxolone inhibits osteoclast formation by suppressing the STING-dependent NF-κB signaling pathway. Omaveloxolone is being investigated for use in ALS, multiple sclerosis, non-alcoholic steatohepatitis, neurodegenerative diseases, and oncology research.
Targets & IC50
Human tumor cells:260 nM (GI50), HT29 cells:1.41 μM (EC50), L929 cells:5.25 μM (EC50), NO:4.4 ± 1.8 nM
In vitro
Methods: HT22 cells were treated with Omaveloxolone (100, 500, 1000 nM) for 24 hours, followed by Western blot analysis for NRF2, HO-1, and NQO1.
Results: Omaveloxolone dose-dependently upregulated NRF2, HO-1, and NQO1 protein levels. [1]
Methods: Human FA patient skin fibroblasts were treated with Omaveloxolone (50 nM) or DMF (10 μM) for 48 hours, followed by DCFDA fluorescence probe detection of reactive oxygen species (ROS) levels.
Results: Omaveloxolone significantly reduced basal ROS levels in FA cells. [2]
In vivo
Methods: 10-month-old APP/PS1 transgenic mice (AD model) and wild-type (WT) controls received intraperitoneal injections of Omaveloxolone (1 mg/kg/day, once daily) for 2 consecutive months.
Results: Omaveloxolone significantly improved the Y-maze alternation rate, number of platform crossings in the water maze, and time spent in the target quadrant in APP/PS1 mice, demonstrating cognitive enhancement.[1]
Methods: Cardio/skeletal muscle-specific FXN knockout mice (FXN-cKO) received oral Omaveloxolone (24 mg/kg/day) mixed with peanut butter from 3 weeks of age until 8 weeks of age (5 weeks total).
Results: Omarsolon significantly improved cardiac function: EF increased from 26% to 47.5% (P<0.001), and FS increased from 22% to 42.5%. [2]
SynonymsRTA-408
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)
Chemical Properties
Molecular Weight554.71
FormulaC33H44F2N2O3
Cas No.1474034-05-3
Smiles[H][C@@]12CC(C)(C)CC[C@@]1(CC[C@]1(C)[C@]2([H])C(=O)C=C2[C@@]1(C)CC[C@@]1([H])C(C)(C)C(=O)C(=C[C@]21C)C#N)NC(=O)C(C)(F)F
Relative Density.1.19 g/cm3 (Predicted)
Storage & Solubility Information
StorageStore at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
Ethanol: 16 mg/mL (28.84 mM), Sonication is recommended.
DMSO: 240 mg/mL (432.66 mM), Sonication is recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble)
In Vivo Formulation
10% DMSO+90% Corn Oil: 3.3 mg/mL (5.95 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM1.8027 mL9.0137 mL18.0274 mL90.1372 mL
5 mM0.3605 mL1.8027 mL3.6055 mL18.0274 mL
10 mM0.1803 mL0.9014 mL1.8027 mL9.0137 mL
20 mM0.0901 mL0.4507 mL0.9014 mL4.5069 mL
DMSO
1mg5mg10mg50mg
50 mM0.0361 mL0.1803 mL0.3605 mL1.8027 mL
100 mM0.0180 mL0.0901 mL0.1803 mL0.9014 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Keywords

Related Tags: Omaveloxolone chemical structure | Omaveloxolone in vivo | Omaveloxolone in vitro | Omaveloxolone formula | Omaveloxolone molecular weight