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Chemical Structure| 218600-44-3 Chemical Structure| 218600-44-3

Structure of Bardoxolone
CAS No.: 218600-44-3

Chemical Structure| 218600-44-3

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CAS No.: 218600-44-3

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Bardoxolone is a nuclear regulator factor (Nrf-2) activator.

Synonyms: CDDO; RTA 401

4.5 *For Research Use Only !

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Product Details of Bardoxolone

CAS No. :218600-44-3
Formula : C31H41NO4
M.W : 491.66
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)O
Synonyms :
CDDO; RTA 401
MDL No. :MFCD07772296

Safety of Bardoxolone

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301
Precautionary Statements:P264-P270-P301+P310-P321-P330-P405-P501
Class:6.1
UN#:2811
Packing Group:Ⅲ

Related Pathways of Bardoxolone

pyroptosis
TLR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
BV2 microglia cell line 10 nM 17 hours Inhibited LPS-induced TNF mRNA expression PMC2396606
Primary microglia 100 nM 24 hours Inhibited LPS-induced TNF and IL-1β mRNA expression PMC2396606
Primary peritoneal macrophages 100 nM 24 hours Inhibited LPS-induced TNF and IL-1β mRNA expression PMC2396606
FET cells 10–300 nM 24 hours CDDO-Me induced the expression of 15-PGDH in a dose-dependent manner and increased 15-PGDH promoter luciferase activity through direct transcriptional regulation. PMC4089461
EL-4, MC38, and LLC tumor cells >1 μM 24 hours To evaluate the direct antitumor effect of CDDO-Me on tumor cells. CDDO-Me showed significant antitumor activity at concentrations higher than 1 μM. PMC2840181
MDSC (Gr-1+CD11b+ cells) 25-100 nM 24 hours To evaluate the effect of CDDO-Me on the immune suppressive activity of MDSC. CDDO-Me significantly increased NQO1 expression, reduced ROS levels, and completely abrogated MDSC-mediated suppression of CD8+ T cell responses. PMC2840181
E18-14C-27 cells 0.3 μmol/L 72 hours Measure cell proliferation, CDDO-Me significantly inhibited cell proliferation PMC5048101
MN9D dopaminergic cell line 10 nM 16-20 hours Inhibited ROS accumulation induced by BV2 microglia conditioned media PMC2396606

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Nrf2+/+ and Nrf2?/? mice Intraperitoneal injection 3 mg/kg Single dose, sacrificed 24 hours later To verify the efficacy of CDDO-Me in inducing Nrf2 signaling in mouse kidneys, immunoblot, qPCR, and immunohistochemical analyses showed upregulation of Nqo1 expression in Nrf2+/+ mice but not in Nrf2?/? mice. PMC4676083
Mice Ang II-induced AAA model Intraperitoneal injection 1.25 mg/kg/day Once daily for 4 weeks To evaluate the effect of BM on AAA progression induced by high ILF3 expression, results showed that BM treatment alleviated the severity of AAA lesions. PMC11344041
Mice Chronic kidney disease model Intraperitoneal injection 10 μmol/kg Daily for 7 days To study the effect of Nrf2 activation on proteinuria, results showed CDDO-Im significantly increased proteinuria PMC7785672
Mice Smad4Tko mice and wild-type mice Oral 250 ng per mouse per day 3 times per week for 1 month CDDO-Me markedly increased survival, reduced inflammation, and inhibited spontaneous colon tumorigenesis. PMC4089461
BALB/c mice Alternaria extract-induced airway inflammation model Intraperitoneal injection 50 μg Once daily for 18 days To evaluate the protective effects of CDDO-Me on airway inflammation, results showed CDDO-Me treatment significantly inhibited Alternaria-induced airway eosinophilia, IL-5 and IL-13 expression, and lung pathological changes. PMC5591045
C57BL/6 mice EL-4 thymoma, LLC lung carcinoma, and MC38 colon carcinoma models Oral 60-150 mg/kg Daily administration for 7-14 days To evaluate the effect of CDDO-Me on MDSC function and tumor growth. CDDO-Me significantly reduced ROS levels in MDSC, eliminated their immune suppressive activity, and delayed tumor growth. In immune-deficient mice, the antitumor effect of CDDO-Me was not significant, indicating that its effect is largely mediated by the immune system. PMC2840181
Mice Spontaneous lupus model Oral gavage 3 mg/kg 3 times per week for 2 months CDDO-Me treatment significantly reduced splenic cellularity, decreased serum autoantibody levels, and attenuated renal disease. PMC4840107
MMTV-neu transgenic mice ER-negative mammary tumor model Oral diet 60 mg/kg diet 45 weeks Prevent ER-negative mammary tumor formation, CDDO-Me significantly delayed tumorigenesis PMC5048101
129/Sv and C57BL/6 female mice Total body irradiation (TBI) model Oral 400 mg/kg diet 3 days To evaluate the protective effect of CDDO-EA against acute gastrointestinal toxicity and DNA damage induced by total body irradiation (TBI). Results showed that CDDO-EA pretreatment significantly improved mouse survival, reduced gastrointestinal damage, and accelerated DNA damage repair. PMC3491493

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00529113 Pancreatic Neoplasms ... More >> Pancreatic Cancer Less << Phase 1 Phase 2 Terminated(To pursue other ind... More >>ications) Less << - United States, Colorado ... More >> Rocky Mountain Cancer Center (US Oncology) Denver, Colorado, United States United States, Florida Cancer Centers of Florida (US Oncology) Ocoee, Florida, United States United States, Indiana Central Indiana Cancer Centers (US Oncology) Indianapolis, Indiana, United States United States, Texas Sammons Cancer Center (US Oncology) Dallas, Texas, United States, 75246 United States, Washington Northwest Cancer Specialist- Vancouver Cancer Specialist (US Oncology) Vancouver, Washington, United States Less <<
NCT01500798 Chronic Kidney Disease ... More >> Type 2 Diabetes Less << Phase 1 Terminated(IDMC recommendation... More >> for safety concerns) Less << - -
NCT01598363 Healthy Volunteers Phase 1 Completed - United States, Wisconsin ... More >> Spaulding Clinical Research, LLC West Bend, Wisconsin, United States, 53095 Less <<
NCT01689116 Healthy Volunteers Phase 1 Completed - United States, Wisconsin ... More >> Spaulding Clinical Research, LLC West Bend, Wisconsin, United States, 53012 Less <<
NCT02316821 Chronic Kidney Disease ... More >> Type 2 Diabetes Less << Phase 2 Completed - Japan ... More >> Tokyo, Japan Less <<
NCT00529438 Advanced Solid Tumors ... More >> Lymphoid Malignancies Less << Phase 1 Completed - United States, Massachusetts ... More >> Beth Israel Deaconess Medical Center Boston, Massachusetts, United States, 02215 United States, Ohio Case Western Reserve University Cleveland, Ohio, United States, 44106 United States, Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 Less <<
NCT01655186 Renal Insufficiency, Chronic ... More >> Diabetes Mellitus, Type 2 Less << Phase 2 Withdrawn(IDMC recommendation ... More >>for safety concerns) Less << October 2013 -
NCT01576887 End-Stage Renal Disease ... More >> Type 2 Diabetes Mellitus Less << Phase 2 Withdrawn(IDMC recommendation ... More >>for safety concerns) Less << October 2013 -
NCT01503866 Healthy Phase 1 Completed - United States, Wisconsin ... More >> Covance Clinical Research Unit Madison, Wisconsin, United States, 53704 Less <<
NCT03550443 Diabetic Kidney Disease Phase 3 Recruiting March 2022 Japan ... More >> Japan Community Health care Organization Sendai Hospital Recruiting Sendai, Miyagi, Japan, 981-0912 Less <<
NCT01551446 Renal Insufficiency, Chronic ... More >> Diabetes Mellitus, Type 2 Less << Phase 1 Withdrawn(IDMC recommendation ... More >>for safety concerns) Less << October 2013 -
NCT00664027 Diabetic Nephropathy Phase 2 Completed - United States, Texas ... More >> West Houston Clinical Research Services Houston, Texas, United States, 77055 Renal Associates, PA San Antonio, Texas, United States, 78215 DGD Research San Antonio, Texas, United States, 78229 Less <<
NCT01351675 Renal Insufficiency, Chronic ... More >> Diabetes Mellitus, Type 2 Less << Phase 3 Terminated(IDMC recommendation... More >> for safety concerns) Less << - -
NCT02036970 Pulmonary Arterial Hypertensio... More >>n Pulmonary Hypertension Interstitial Lung Disease Idiopathic Interstitial Pneumonia Idiopathic Pulmonary Fibrosis Sarcoidosis Respiratory Bronchiolitis Associated Interstitial Lung Disease Desquamative Interstitial Pneumonia Cryptogenic Organizing Pneumonia Acute Interstitial Pneumonitis Idiopathic Lymphoid Interstitial Pneumonia Idiopathic Pleuroparenchymal Fibroelastosis Less << Phase 2 Completed - -
NCT01549769 Renal Insufficiency, Chronic ... More >> Diabetes Mellitus, Type 2 Less << Phase 1 Terminated(IDMC recommendation... More >> for safety concerns) Less << - -
NCT00811889 Chronic Kidney Disease ... More >> Type 2 Diabetes Diabetic Nephropathy Less << Phase 2 Completed - -
NCT01053936 Renal Insufficiency, Chronic ... More >> Diabetes Mellitus, Type 2 Less << Phase 2 Completed - -
NCT01461161 Healthy Volunteers Phase 1 Completed - United States, Wisconsin ... More >> Spaulding Clinical Research West Bend, Wisconsin, United States, 53095 Less <<
NCT02657356 Connective Tissue Disease-Asso... More >>ciated Pulmonary Arterial Hypertension Less << Phase 3 Recruiting June 2020 -
NCT03264079 Healthy Volunteers Phase 1 Completed - United States, Ohio ... More >> Medpace Clinical Pharmacology Unit Cincinnati, Ohio, United States, 45227 Less <<
NCT03019185 Alport Syndrome Phase 2 Phase 3 Active, not recruiting December 2020 -
NCT03068130 Pulmonary Hypertension Phase 3 Recruiting December 2021 -
NCT03749447 Chronic Kidney Diseases ... More >> Alport Syndrome Less << Phase 3 Not yet recruiting February 2024 -
NCT01563562 Hepatic Impairment ... More >> Healthy Less << Phase 1 Completed - United States, Florida ... More >> University of Miami School of Medicine Miami, Florida, United States, 33136 United States, North Carolina Duke University Durham, North Carolina, United States, 27710 Less <<
NCT03366337 IgA Nephropathy ... More >> CKD Associated With Type 1 Diabetes Focal Segmental Glomerulosclerosis Autosomal Dominant Polycystic Kidney Less << Phase 2 Recruiting August 2019 -
NCT00322140 Solid Tumors|Lymphoma PHASE1 COMPLETED 2008-01-14 National Institutes of Health ... More >>Clinical Center, 9000 Rockville Pike, Bethesda, Maryland, 20892, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.17mL

2.03mL

1.02mL

20.34mL

4.07mL

2.03mL
Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

Historical Records

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