Bardoxolone

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[1][2].

Product Specifications

CAS Number

[218600-44-3]

Product Name Alternative

CDDO; RTA 401

UNSPSC

12352211

Hazard Statement

H302, H315, H319, H335

Target

Keap1-Nrf2; Necroptosis; SARS-CoV; Virus Protease

Type

Reference compound

Related Pathways

Anti-infection; Apoptosis; NF-κB

Applications

Cancer-Kinase/protease

Field of Research

Infection; Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/Bardoxolone.html

Concentration

10mM

Purity

99.50

Solubility

DMSO : 100 mg/mL (ultrasonic)

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

Molecular Formula

C31H41NO4

Molecular Weight

491.66

Precautions

H302, H315, H319, H335

References & Citations

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