Bardoxolone methyl (Synonyms: RTA 402; NSC 713200; CDDO Methyl ester)

Name: Bardoxolone methyl
Brand: MedChemExpress
SKU: HY-13324
Rating: 5.0 (29 reviews)

Cat. No.: HY-13324 Purity: 98.92%: FAQs
Data Sheet SDS COA Handling Instructions

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Bardoxolone methyl (NSC 713200; RTA 402; CDDO Methyl ester) is a synthetic triterpenoid compound with potential antineoplastic and anti-inflammatory activities, acting as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway.

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

Bardoxolone methyl Chemical Structure

CAS No. : 218600-53-4

Size	Stock	Quantity
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	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 29 publication(s) in Google Scholar

Other Forms of Bardoxolone methyl:

Bardoxolone In-stock

28 Publications Citing Use of MCE Bardoxolone methyl

: Bardoxolone methyl purchased from MedChemExpress. Usage Cited in: Toxicol Lett. 2016 Sep 30;259:52-59. [Abstract]; MATE1/SCL47A1 efflux transporter expression in hPTCs. Protein (n=3) expression is assessed after administration of NSC 119875 and pre- or delayedexposure to CDDO-Me after 12 h. GAPDH is used as a housekeeping gene. β-actin is used as a loading control.

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Biological Activity
Protocol
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References
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Description

IC₅₀ & Target

Nrf2^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.36 μM Compound: CDDO-Me	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31051401]
A549	IC₅₀	0.52 μM Compound: CDDO-Me	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 31725288]
A549	IC₅₀	0.63 μM Compound: CDDO-Me	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35238566]
A549	IC₅₀	2.074 μM Compound: CDDO-Me	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 29501947]
A549/TR	IC₅₀	1.703 μM Compound: CDDO-Me	Antiproliferative activity against human A549/TR cells after 72 hrs by MTT assay Antiproliferative activity against human A549/TR cells after 72 hrs by MTT assay	[PMID: 29501947]
B16-F10	IC₅₀	5.85 μM Compound: CDDO-Me	Cytotoxicity against mouse B16F10 cells after 48 hrs by MTT assay Cytotoxicity against mouse B16F10 cells after 48 hrs by MTT assay	[PMID: 24685545]
CCD-841CoN	IC₅₀	0.316 μM Compound: CDDO-Me	Antiproliferative activity against human CCD-841-CoN cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Antiproliferative activity against human CCD-841-CoN cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 25675144]
H9c2	IC₅₀	5.2 μM Compound: CDDO-Me	Cytotoxicity against rat H9c2 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against rat H9c2 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 28994286]
HCT-116	IC₅₀	0.25 nM Compound: CDDO-Me	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay	[PMID: 30429953]
HCT-116	IC₅₀	0.84 μM Compound: CDDO-Me	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35238566]
HCT-8	IC₅₀	0.29 μM Compound: CDDO-Me	Antiproliferative activity against human HCT8 cells after 72 hrs by SRB assay Antiproliferative activity against human HCT8 cells after 72 hrs by SRB assay	[PMID: 30429953]
HCT-8	IC₅₀	0.363 μM Compound: CDDO-Me	Antiproliferative activity against 5-FU resistant human HCT8 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Antiproliferative activity against 5-FU resistant human HCT8 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 25675144]
HCT-8	IC₅₀	0.399 μM Compound: CDDO-Me	Antiproliferative activity against human HCT8 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Antiproliferative activity against human HCT8 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 25675144]
HEK293	IC₅₀	2.2 μM Compound: CDDO-Me	Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 28994286]
HepG2	IC₅₀	0.26 μM Compound: CDDO-Me	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31051401]
HepG2	IC₅₀	0.52 μM Compound: CDDO-Me	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 31725288]
HepG2	IC₅₀	4.99 μM Compound: CDDO-Me	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 24685545]
HOS	IC₅₀	0.66 μM Compound: CDDO-Me	Antiproliferative activity against human HOS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human HOS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 31725288]
HT-29	IC₅₀	0.28 μM Compound: CDDO-Me	Antiproliferative activity against human HT-29 cells after 72 hrs by SRB assay Antiproliferative activity against human HT-29 cells after 72 hrs by SRB assay	[PMID: 30429953]
HT-29	EC₅₀	4.34 μM Compound: 10; CDDO-Me	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: 10; CDDO-Me	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	0.2 nM Compound: CDDO-Me	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	IC₅₀	0.35 μM Compound: CDDO-Me	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31051401]
MCF7	IC₅₀	0.85 μM Compound: CDDO-Me	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 31725288]
MDA-MB-231	IC₅₀	0.56 μM Compound: CDDO-Me	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35238566]
U2OS	IC₅₀	0.74 μM Compound: CDDO-Me	Antiproliferative activity against human U2OS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human U2OS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35238566]

In Vivo

Bardoxolone methyl (30 mg/kg, p.o.) decreases renal expression of megalin but not cubilin, increases creatinine clearance and urinary albumin-to-creatinine ratios, and induces Nrf2 cytoprotective targets in cynomolgus monkeys^[1]. Bardoxolone methyl induces overall favorable effects on the heart via its improvement in eGFR in both animal models and clinical trials^[2].

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

Clinical Trial

Molecular Weight

505.69

Formula

C₃₂H₄₃NO₄

CAS No.

218600-53-4

Appearance

Solid

Color

White to yellow

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)(C(OC)=O)CC3)(C)C2=CC4=O)([H])C1(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (49.44 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	1.9775 mL	9.8875 mL	19.7750 mL
5 mM	0.3955 mL	1.9775 mL	3.9550 mL
10 mM	0.1977 mL	0.9887 mL	1.9775 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, 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.

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 (4.94 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 (4.94 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.
Protocol 3

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: 2.5 mg/mL (4.94 mM); Suspended solution; Need ultrasonic

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: Corn Oil
Solubility: 5 mg/mL (9.89 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (19.77 mM); Suspended solution; Need ultrasonic and warming and heat to 40°C

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: 99.31%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (254 KB) HNMR (217 KB) LCMS (120 KB)

Handling Instructions (2659 KB)

References

[1]. Reisman SA, et al. Bardoxolone Methyl Decreases Megalin and Activates Nrf2 in the Kidney. J Am Soc Nephrol. 2012 Aug 2. [Content Brief]

[2]. McCullough PA, et al. Cardiac and renal function in patients with type 2 diabetes who have chronic kidney disease: potential effects of bardoxolone methyl. Drug Des Devel Ther. 2012;6:141-9. [Content Brief]

Animal Administration
^[1]

Two separate in-life studies are conducted in cynomolgus monkeys. In one study, cynomolgus monkeys (n=9/gender/dose group) are administered amorphous bardoxolone methyl by oral gavage, using sesame oil as the vehicle, at 5, 30, and 300 mg/kg once daily for 12 months in a GLP environment. Observations for morbidity, mortality, injury, and the availability of food and water are conducted twice daily for all animals. Clinical observations and body weights are conducted and recorded weekly. Weight data are analyzed by calculating the area under the weight versus time curve using the linear trapezoidal method. Blood samples for clinical chemistry evaluations are collected from all animals pretest and from all animals prior to interim (6-month) and terminal (12-month) necropsies. An additional group of monkeys for each dose group are allowed to recover for 4 weeks.

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

References

[1]. Reisman SA, et al. Bardoxolone Methyl Decreases Megalin and Activates Nrf2 in the Kidney. J Am Soc Nephrol. 2012 Aug 2. [Content Brief]

[2]. McCullough PA, et al. Cardiac and renal function in patients with type 2 diabetes who have chronic kidney disease: potential effects of bardoxolone methyl. Drug Des Devel Ther. 2012;6:141-9. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.9775 mL	9.8875 mL	19.7750 mL	49.4374 mL
	5 mM	0.3955 mL	1.9775 mL	3.9550 mL	9.8875 mL
	10 mM	0.1977 mL	0.9887 mL	1.9775 mL	4.9437 mL
	15 mM	0.1318 mL	0.6592 mL	1.3183 mL	3.2958 mL
	20 mM	0.0989 mL	0.4944 mL	0.9887 mL	2.4719 mL
	25 mM	0.0791 mL	0.3955 mL	0.7910 mL	1.9775 mL
	30 mM	0.0659 mL	0.3296 mL	0.6592 mL	1.6479 mL
	40 mM	0.0494 mL	0.2472 mL	0.4944 mL	1.2359 mL

Bardoxolone methyl Related Classifications

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:

Bardoxolone methyl218600-53-4RTA 402 NSC 713200 CDDO Methyl esterRTA402RTA-402NSC713200NSC 713200NSC-713200Keap1-Nrf2AutophagyApoptosisFerroptosisInhibitorinhibitorinhibit

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Bardoxolone methyl (Synonyms: RTA 402; NSC 713200; CDDO Methyl ester)

Customer Review

Other Forms of Bardoxolone methyl:

Bardoxolone methyl Related Antibodies

28 Publications Citing Use of MCE Bardoxolone methyl

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Biological Activity

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References

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Complete Stock Solution Preparation Table

Bardoxolone methyl Related Classifications

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