bardoxolone

Ligand id: 2717

Name: bardoxolone

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 5
Hydrogen bond donors 1
Rotatable bonds 1
Topological polar surface area 95.23
Molecular weight 491.3
XLogP 6.3
No. Lipinski's rules broken 1

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Clinical trials for treatment of chronic kidney disease (CKD) as a result of type 2 diabetes mellitus have been terminated. Visit ClinicalTrials.gov to view currently registered drug trials involving this compound.
Mechanism Of Action and Pharmacodynamic Effects
Bardoxolone inhibits the ubiquitinisation activity of KEAP1, a protein which interacts with and ubiquitinises the Nrf2 transcription factor (NFE2L2, Q16236) and sequesters Nrf2 to the cytoplasm. Bardoxolone-induced activation of Nrf2 leads to activation of Keap1-Nrf2 pathway which regulates genes (containing antioxidant response elements (AREs)) involved in antioxidant and anti-inflammatory responses [1-2,4].