Omaveloxolone (RTA-408)

Catalog No.S7672

For research use only.

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

Omaveloxolone (RTA-408) Chemical Structure

CAS No. 1474034-05-3

Selleck's Omaveloxolone (RTA-408) has been cited by 4 Publications

Purity & Quality Control

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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 [1]
()
Nrf2 [1]
()
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]

Protocol (from reference)

Cell Research:[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 Research:[2]
  • Animal Models: Mice with radiation-induced dermatitis
  • Dosages: 1% in 100 μL vehicle (w/v)
  • Administration: Topical application

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(180.27 mM)
Ethanol 20 mg/mL
(36.05 mM)
Water Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
10%DMSO+90% Corn oil
For best results, use promptly after mixing.

30mg/mL

Chemical Information

Molecular Weight 554.71
Formula

C33H44F2N2O3

CAS No. 1474034-05-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1(CCC2(CCC3(C(C2C1)C(=O)C=C4C3(CCC5C4(C=C(C(=O)C5(C)C)C#N)C)C)C)NC(=O)C(C)(F)F)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03902002 Completed Drug: Omaveloxolone 50 mg capsules Hepatic Impairment Reata Pharmaceuticals Inc. July 19 2019 Phase 1
NCT03931590 Completed Drug: [14C]-Omaveloxolone Healthy Male Subjects Reata Pharmaceuticals Inc. April 11 2019 Phase 1
NCT03664453 Completed Drug: omaveloxolone Healthy Reata Pharmaceuticals Inc. October 29 2018 Phase 1
NCT02029716 Completed Drug: RTA 408 Lotion 0.5% 1% 3%|Drug: Lotion vehicle/placebo Healthy Reata Pharmaceuticals Inc.|AbbVie December 2013 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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