Bardoxolone (Synonyms: CDDO; RTA 401)

Name: Bardoxolone
Brand: MedChemExpress
SKU: HY-14909
Rating: 5.0 (17 reviews)

Cat. No.: HY-14909 Purity: 99.50%: Data Sheet
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Bardoxolone (RTA 401; CDDO) is an orally active activator of nuclear regulatory factor (NRf-2) and an inhibitor of SARS-CoV-2 3CL protease. Bardoxolone inhibits SARS-CoV-2 3CL protease with an EC₅₀ value of 0.43 μM in vero cells. Bardoxolone also inhibits necroptosis in HT-29 cells with an EC₅₀ value of 1.30 μM by blocking necrosome formation through inhibiting phosphorylation of RIPK1 and RIPK3. Bardoxolone can be used in research on COVID-19, TNF-induced systemic inflammatory response syndrome (SIRS), and cerebral ischemia-reperfusion injury.

For research use only. We do not sell to patients.

Bardoxolone Chemical Structure

CAS No. : 218600-44-3

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of Bardoxolone:

Bardoxolone methyl In-stock
Bardoxolone (Standard) Get quote

17 Publications Citing Use of MCE Bardoxolone

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Nrf-2^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HT-29	EC₅₀	1.3 μM Compound: 7; CDDO	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	> 10 μM Compound: 7; CDDO	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]
Macrophage	IC₅₀	0.0004 μM Compound: 4, CDDO	Antiinflammatory activity in mouse macrophages assessed as inhibition of IFN-gamma-induced nitric oxide production after 48 hrs by Griess method Antiinflammatory activity in mouse macrophages assessed as inhibition of IFN-gamma-induced nitric oxide production after 48 hrs by Griess method	[PMID: 23837912]
Macrophage	IC₅₀	0.5 nM Compound: CDDO	Antiinflammatory activity in CD-1 mouse Macrophage assessed as inhibition of IFN-gamma induced NO production after 48 hrs by Griess reaction Antiinflammatory activity in CD-1 mouse Macrophage assessed as inhibition of IFN-gamma induced NO production after 48 hrs by Griess reaction	[PMID: 21361338]
Macrophage	IC₅₀	4.3 nM Compound: CDDO	Antiinflammatory activity in CD-1 mouse Macrophage assessed as inhibition of IFN-gamma induced NO production after 48 hrs by Griess reaction Antiinflammatory activity in CD-1 mouse Macrophage assessed as inhibition of IFN-gamma induced NO production after 48 hrs by Griess reaction	[PMID: 21361338]
MCF7	EC₅₀	0.16 μM Compound: CDDO	Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 3 days by radioactive thymidine incorporation assay Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 3 days by radioactive thymidine incorporation assay	[PMID: 26177446]
RAW	IC₅₀	20 nM Compound: CDDO	Inhibition of interferon gamma-stimulated NO production in RAW 264.7 cells after 24 hrs Inhibition of interferon gamma-stimulated NO production in RAW 264.7 cells after 24 hrs	[PMID: 17367124]
RAW264.7	IC₅₀	11 nM Compound: CDDO, Bardoxolone	Inhibition of NO production in INFgamma-stimulated mouse RAW264.7 cells measured after 24 hrs by Griess reaction method Inhibition of NO production in INFgamma-stimulated mouse RAW264.7 cells measured after 24 hrs by Griess reaction method	[PMID: 21441026]
RAW264.7	IC₅₀	16.5 nM Compound: CDDO	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFNgamma-stimulated NO production pretreated for 2 hrs before IFNgamma challenge measured after 24 hrs by Griess reaction Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFNgamma-stimulated NO production pretreated for 2 hrs before IFNgamma challenge measured after 24 hrs by Griess reaction	[PMID: 22533790]
RAW264.7	IC₅₀	17 nM Compound: CDDO	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFN-gamma induced NO production after 24 hrs by Griess reaction Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFN-gamma induced NO production after 24 hrs by Griess reaction	[PMID: 21361338]
RAW264.7	IC₅₀	23 nM Compound: CDDO	Inhibition of iNOS in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of nitric oxide production after 48 hrs by Griess assay Inhibition of iNOS in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of nitric oxide production after 48 hrs by Griess assay	[PMID: 25965897]
RAW264.7	IC₅₀	28.3 nM Compound: CDDO	Antiinflammatory activity against IFN-gamma-stimulated mouse RAW264.7 cells assessed as nitrite accumulation after 24 hrs by Griess reagent method Antiinflammatory activity against IFN-gamma-stimulated mouse RAW264.7 cells assessed as nitrite accumulation after 24 hrs by Griess reagent method	[PMID: 20188548]

Clinical Trial

Molecular Weight

491.66

Formula

C₃₁H₄₁NO₄

CAS No.

218600-44-3

Appearance

Solid

Color

White to yellow

SMILES

CC1(C)CC[C@@]2(C(O)=O)[C@@]([C@](C(C=C3[C@@]4(C)CC[C@]5([H])[C@]3(C)C=C(C#N)C(C5(C)C)=O)=O)([H])[C@@]4(C)CC2)([H])C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (203.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0339 mL	10.1696 mL	20.3393 mL
5 mM	0.4068 mL	2.0339 mL	4.0679 mL
10 mM	0.2034 mL	1.0170 mL	2.0339 mL

View the 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.08 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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.50%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (252 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Sun Q, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212. [Content Brief]

[2]. Wang Y, et al. Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors. Eur J Med Chem. 2021 Feb 15;212:113030. [Content Brief]

Animal Administration
^[3]^[4]

Monkeys^[3]
Two separate studies are conducted in cynomolgus Monkeys. In one, cynomolgus Monkeys (n=9 per sex/dose group) are orally administered Bardoxolone methyl at 5, 30, and 300 mg/kg once daily for 12 months, with an interim analysis at 6 months and a postdose recovery analysis 4 weeks after the final dose, in a GLP environment. In a second study, female cynomolgus Monkeys (n=6 for vehicle and n=12 for treatment) are administered Bardoxolone methyl (30 mg/kg per day), as above, once daily for 28 days.
Mice^[4]
Male C57BL/6J mice are used. After 1 week of acclimatisation to the institutional animal facility (temperature 22°C, 12 h light/dark cycle), the animals are divided into three groups (n=7): (1) mice fed a normal diet (LFD group); (2) mice fed a high-fat diet (HFD group) (40% fat); and (3) mice fed the same HFD and supplemented with BARD in drinking water (10 mg/kg body weight) (HFD/BARD group). The dose and oral administration of BARD are chosen. After 21 weeks, all mice are euthanized using CO2 asphyxiation. Part of the mesenteric fat mass in each animal is collected and stored at −80°C for Western blot analysis. Another portion of the mesenteric fat depot is fixed in 4% paraformaldehyde and embedded in paraffin for the determination of morphology and immunohistochemistry.

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

References

[1]. Sun Q, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212. [Content Brief]

[2]. Wang Y, et al. Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors. Eur J Med Chem. 2021 Feb 15;212:113030. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0339 mL	10.1696 mL	20.3393 mL	50.8481 mL
	5 mM	0.4068 mL	2.0339 mL	4.0679 mL	10.1696 mL
	10 mM	0.2034 mL	1.0170 mL	2.0339 mL	5.0848 mL
	15 mM	0.1356 mL	0.6780 mL	1.3560 mL	3.3899 mL
	20 mM	0.1017 mL	0.5085 mL	1.0170 mL	2.5424 mL
	25 mM	0.0814 mL	0.4068 mL	0.8136 mL	2.0339 mL
	30 mM	0.0678 mL	0.3390 mL	0.6780 mL	1.6949 mL
	40 mM	0.0508 mL	0.2542 mL	0.5085 mL	1.2712 mL
	50 mM	0.0407 mL	0.2034 mL	0.4068 mL	1.0170 mL
	60 mM	0.0339 mL	0.1695 mL	0.3390 mL	0.8475 mL
	80 mM	0.0254 mL	0.1271 mL	0.2542 mL	0.6356 mL
	100 mM	0.0203 mL	0.1017 mL	0.2034 mL	0.5085 mL

Bardoxolone Related Classifications

Inflammation/Immunology Infection Cardiovascular Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Bardoxolone218600-44-3CDDO RTA 401RTA401RTA 401RTA-401Keap1-Nrf2NecroptosisSARS-CoVVirus ProteaseSARS coronavirusNRf-2SARS-CoV-2 3CL proteaseHsp90necroptosisInhibitorinhibitorinhibit

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Bardoxolone (Synonyms: CDDO; RTA 401)

Customer Review

Other Forms of Bardoxolone:

Bardoxolone Related Antibodies

17 Publications Citing Use of MCE Bardoxolone

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

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Complete Stock Solution Preparation Table

Bardoxolone Related Classifications

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