Omaveloxolone (RTA-408) | NRF2 Activator | CAS 1474034-05-3

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Quality Control

Batch: Purity: 99.91%

99.91

Related Targets	HDAC Antioxidant ROS IκB/IKK Nrf2 AP-1 MALT NOD
Other NF-κB Inhibitors	DCZ0415 BAY 11-7082 (BAY 11-7821) JSH-23 QNZ (EVP4593) Caffeic Acid Phenethyl Ester SC75741 DHA (Dihydroartemisinin) Withaferin A (WFA) Andrographolide Evodiamine

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (180.27 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.25mg/ml (2.25mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.7mg/ml (1.26mM)	Taking the 1 mL working solution as an example, add 50 μL of 14 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.

Chemical Information, Storage & Stability

Molecular Weight	554.71	Formula	C₃₃H₄₄F₂N₂O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1474034-05-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			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

Mechanism of Action

Targets/IC₅₀/Ki	NF-κB Nrf2
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.
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. In rat skin, RTA 408 activates Nrf2 and induces cytoprotective genes. RTA 408 also mitigates hematopoietic acute radiation syndrome in mice.
References	[1] https://pubmed.ncbi.nlm.nih.gov/25897966/ [2] https://pubmed.ncbi.nlm.nih.gov/24720753/ [3] https://pubmed.ncbi.nlm.nih.gov/24362512/ [4] https://pubmed.ncbi.nlm.nih.gov/25738896/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06054893	Not yet recruiting	Friedreich Ataxia	Biogen	November 1 2023	Phase 1
NCT05909644	Completed	Healthy Adult Subjects	Reata a wholly owned subsidiary of Biogen\|Celerion\|Q2 Solutions\|Altasciences Company Inc.\|Biogen	July 5 2023	Phase 1
NCT03902002	Completed	Hepatic Impairment	Reata a wholly owned subsidiary of Biogen\|Biogen	July 19 2019	Phase 1
NCT03931590	Completed	Healthy Male Subjects	Reata a wholly owned subsidiary of Biogen\|Biogen	April 11 2019	Phase 1
NCT03664453	Completed	Healthy	Reata a wholly owned subsidiary of Biogen\|Biogen	October 29 2018	Phase 1

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Omaveloxolone (RTA-408) NRF2 activator

Chemical Structure

Molecular Weight: 554.71