Bardoxolone methyl

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MedKoo CAT#: 202530

CAS#: 218600-53-4

Description: Bardoxolone methyl (also known as “RTA 402” and “CDDO-methyl ester”) is an orally-available first-in-class synthetic triterpenoid belonging to the antioxidant inflammation modulator (AIM) class. It is the most potent known inducer of the Nrf2 pathway to enter clinical development and works to suppress both oxidative stress and inflammation. Bardoxolone methyl is currently being developed by Reata Pharmaceuticals, Inc. in partnership with Abbott Laboratories and Kyowa Hakko Kirin, for the treatment of advanced chronic kidney disease (CKD) in type 2 diabetes mellitus patients.

Chemical Structure

Bardoxolone methyl
CAS# 218600-53-4

Theoretical Analysis

MedKoo Cat#: 202530
Name: Bardoxolone methyl
CAS#: 218600-53-4
Chemical Formula: C32H43NO4
Exact Mass: 505.31921
Molecular Weight: 505.69
Elemental Analysis: C, 76.00; H, 8.57; N, 2.77; O, 12.66

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Size Price Availability Quantity
100.0mg USD 150.0 Same Day
200.0mg USD 250.0 Same Day
500.0mg USD 550.0 Same Day
1.0g USD 950.0 Same Day
2.0g USD 1710.0 Same Day
5.0g USD 2950.0 2 Weeks
10.0g USD 5310.0 2 Weeks
20.0g USD 8750.0 2 Weeks
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Synonym: Bardoxolone methyl; CDDO Methyl ester; CDDOMe; NSC 713200; RTA 402; RTA-402; RTA402; TP-155; TP155; TP 155

IUPAC/Chemical Name: (4aS,6aR,6bS,12aS,14aR,14bR)-methyl 11-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,12a,14,14a,14b-octadecahydropicene-4a-carboxylate


InChi Code: InChI=1S/C32H43NO4/c1-27(2)11-13-32(26(36)37-8)14-12-31(7)24(20(32)17-27)21(34)15-23-29(5)16-19(18-33)25(35)28(3,4)22(29)9-10-30(23,31)6/h15-16,20,22,24H,9-14,17H2,1-8H3/t20-,22?,24+,29+,30-,31-,32+/m1/s1

SMILES Code: O=C([C@]1(CC[C@@]2(C)[C@]3(C)CCC4C(C)(C)C(C(C#N)=C[C@]4(C)C3=C5)=O)CCC(C)(C)C[C@]1([H])[C@@]2([H])C5=O)OC

Appearance: White to off-white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 505.69 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Hermann C, Lang S, Popp T, Hafner S, Steinritz D, Rump A, Port M, Eder S. Bardoxolone-Methyl (CDDO-Me) Impairs Tumor Growth and Induces Radiosensitization of Oral Squamous Cell Carcinoma Cells. Front Pharmacol. 2021 Jan 29;11:607580. doi: 10.3389/fphar.2020.607580. PMID: 33584286; PMCID: PMC7878525.

2: Yamazaki T, Mimura I, Tanaka T, Nangaku M. Treatment of Diabetic Kidney Disease: Current and Future. Diabetes Metab J. 2021 Jan;45(1):11-26. doi: 10.4093/dmj.2020.0217. Epub 2021 Jan 22. PMID: 33508907; PMCID: PMC7850867.

3: Pedrosa AL, Bitencourt L, Paranhos RM, Leitão CA, Ferreira GC, Simões E Silva AC. Alport Syndrome: a comprehensive review on genetics, pathophysiology, histology, clinical, and therapeutic perspectives. Curr Med Chem. 2021 Jan 7. doi: 10.2174/0929867328666210108113500. Epub ahead of print. PMID: 33423643.

4: Sakuma H, Hagiwara S, Kantharidis P, Gohda T, Suzuki Y. Potential Targeting of Renal Fibrosis in Diabetic Kidney Disease Using MicroRNAs. Front Pharmacol. 2020 Nov 13;11:587689. doi: 10.3389/fphar.2020.587689. PMID: 33364960; PMCID: PMC7751689.

5: Wang Y, Ma H, Huang J, Yao Z, Yu J, Zhang W, Zhang L, Wang Z, Zhuang C. Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors. Eur J Med Chem. 2021 Feb 15;212:113030. doi: 10.1016/j.ejmech.2020.113030. Epub 2020 Nov 21. PMID: 33248849.

6: Baran SW, Gupta AD, Lim MA, Mathur A, Rowlands DJ, Schaevitz LR, Shanmukhappa SK, Walker DB. Continuous, Automated Breathing Rate and Body Motion Monitoring of Rats With Paraquat-Induced Progressive Lung Injury. Front Physiol. 2020 Oct 16;11:569001. doi: 10.3389/fphys.2020.569001. PMID: 33178039; PMCID: PMC7596732.

7: Szczesny-Malysiak E, Stojak M, Campagna R, Grosicki M, Jamrozik M, Kaczara P, Chlopicki S. Bardoxolone Methyl Displays Detrimental Effects on Endothelial Bioenergetics, Suppresses Endothelial ET-1 Release, and Increases Endothelial Permeability in Human Microvascular Endothelium. Oxid Med Cell Longev. 2020 Oct 14;2020:4678252. doi: 10.1155/2020/4678252. PMID: 33123312; PMCID: PMC7584962.

8: Rice CA, Colon BL, Chen E, Hull MV, Kyle DE. Discovery of repurposing drug candidates for the treatment of diseases caused by pathogenic free-living amoebae. PLoS Negl Trop Dis. 2020 Sep 24;14(9):e0008353. doi: 10.1371/journal.pntd.0008353. PMID: 32970675; PMCID: PMC7546510.

9: Tong B, Luo M, Xie Y, Spradlin JN, Tallarico JA, McKenna JM, Schirle M, Maimone TJ, Nomura DK. Bardoxolone conjugation enables targeted protein degradation of BRD4. Sci Rep. 2020 Sep 23;10(1):15543. doi: 10.1038/s41598-020-72491-9. PMID: 32968148; PMCID: PMC7511954.

10: Tian TT, Li QR, Gan SQ, Chang CR, Shen XC. Protective Effect of Simplicillium sp. Ethyl Acetate Extract against High Glucose-Induced Oxidative Stress in HUVECs. Evid Based Complement Alternat Med. 2020 Aug 15;2020:5172765. doi: 10.1155/2020/5172765. PMID: 32879632; PMCID: PMC7448235.

11: Lewis JH, Jadoul M, Block GA, Chin MP, Ferguson DA, Goldsberry A, Meyer CJ, O'Grady M, Pergola PE, Reisman SA, Wigley WC, Chertow GM. Effects of Bardoxolone Methyl on Hepatic Enzymes in Patients with Type 2 Diabetes Mellitus and Stage 4 CKD. Clin Transl Sci. 2021 Jan;14(1):299-309. doi: 10.1111/cts.12868. Epub 2020 Sep 3. PMID: 32860734; PMCID: PMC7877861.

12: Rush BM, Bondi CD, Stocker SD, Barry KM, Small SA, Ong J, Jobbagy S, Stolz DB, Bastacky SI, Chartoumpekis DV, Kensler TW, Tan RJ. Genetic or pharmacologic Nrf2 activation increases proteinuria in chronic kidney disease in mice. Kidney Int. 2021 Jan;99(1):102-116. doi: 10.1016/j.kint.2020.07.036. Epub 2020 Aug 18. PMID: 32818518; PMCID: PMC7785672.

13: Meng X, Waddington JC, Tailor A, Lister A, Hamlett J, Berry N, Park BK, Sporn MB. CDDO-imidazolide Targets Multiple Amino Acid Residues on the Nrf2 Adaptor, Keap1. J Med Chem. 2020 Sep 10;63(17):9965-9976. doi: 10.1021/acs.jmedchem.0c01088. Epub 2020 Aug 19. PMID: 32787104.

14: Yagishita Y, Gatbonton-Schwager TN, McCallum ML, Kensler TW. Current Landscape of NRF2 Biomarkers in Clinical Trials. Antioxidants (Basel). 2020 Aug 7;9(8):716. doi: 10.3390/antiox9080716. PMID: 32784785; PMCID: PMC7464243.

15: Kim J, Hagen CE, Kumar SN, Park JI, Zimmerman MA, Hong JC. Anticholestatic Effect of Bardoxolone Methyl on Hepatic Ischemia-reperfusion Injury in Rats. Transplant Direct. 2020 Jul 17;6(8):e584. doi: 10.1097/TXD.0000000000001017. PMID: 32766432; PMCID: PMC7371100.

16: Cuadrado A, Pajares M, Benito C, Jiménez-Villegas J, Escoll M, Fernández- Ginés R, Garcia Yagüe AJ, Lastra D, Manda G, Rojo AI, Dinkova-Kostova AT. Can Activation of NRF2 Be a Strategy against COVID-19? Trends Pharmacol Sci. 2020 Sep;41(9):598-610. doi: 10.1016/ Epub 2020 Jul 14. PMID: 32711925; PMCID: PMC7359808.

17: Kanda H, Yamawaki K. Bardoxolone methyl: drug development for diabetic kidney disease. Clin Exp Nephrol. 2020 Oct;24(10):857-864. doi: 10.1007/s10157-020-01917-5. Epub 2020 Jun 27. PMID: 32594372; PMCID: PMC7497696.

18: Harrington BS, Ozaki MK, Caminear MW, Hernandez LF, Jordan E, Kalinowski NJ, Goldlust IS, Guha R, Ferrer M, Thomas C, Shetty J, Tran B, Wong N, House CD, Annunziata CM. Drugs Targeting Tumor-Initiating Cells Prolong Survival in a Post-Surgery, Post-Chemotherapy Ovarian Cancer Relapse Model. Cancers (Basel). 2020 Jun 21;12(6):1645. doi: 10.3390/cancers12061645. PMID: 32575908; PMCID: PMC7352549.

19: Kalvala AK, Kumar R, Sherkhane B, Gundu C, Arruri VK, Kumar A. Bardoxolone Methyl Ameliorates Hyperglycemia Induced Mitochondrial Dysfunction by Activating the keap1-Nrf2-ARE Pathway in Experimental Diabetic Neuropathy. Mol Neurobiol. 2020 Aug;57(8):3616-3631. doi: 10.1007/s12035-020-01989-0. Epub 2020 Jun 19. PMID: 32556916.

20: Nangaku M, Kanda H, Takama H, Ichikawa T, Hase H, Akizawa T. Randomized Clinical Trial on the Effect of Bardoxolone Methyl on GFR in Diabetic Kidney Disease Patients (TSUBAKI Study). Kidney Int Rep. 2020 Apr 14;5(6):879-890. doi: 10.1016/j.ekir.2020.03.030. PMID: 32518870; PMCID: PMC7271944.

Additional Information

Bardoxolone methyl, previously known as RTA 402, is the lead molecule emerging from ReataÂ’s platform of Antioxidant Inflammation Modulators (AIMs). The AIMs are the most potent known inducers of Nrf2, an important emerging biological target that controls the production of many of the bodyÂ’s antioxidant and detoxification enzymes. There is a strong biological rationale for the use of agents targeting Nrf2 to treat renal and cardiovascular disease. Chronic oxidative stress-mediated inflammation is known to play an important role in the degeneration of kidney function. Based on data from three clinical studies demonstrating improvements in patientsÂ’ markers of kidney function and potential disease-modifying activity, bardoxolone has been advanced to late-stage clinical development and is currently undergoing a pivotal Phase 2b trial in chronic kidney disease patients with type 2 diabetes mellitus.