Bardoxolone

SKU: orb1304848

Description

Bardoxolone methyl is a potent synthetic triterpenoid that activates the Nrf2 pathway and inhibits NF-κB signaling, leading to antioxidant and anti-inflammatory effects. It has been investigated in vitro for cancer research by inducing apoptosis and in vivo for conditions like chronic kidney disease and pulmonary arterial hypertension.

Research Area

Cell Biology, Immunology & Inflammation, Infectious Disease & Virology

Key Properties

• CAS Number: 218600-44-3
• MW: 491.66
• Purity: 99.19% (May vary between batches)
• Formula: C₃₁H₄₁NO₄
• SMILES: CC1(C)CC[C@@]2(CC[C@]3(C)[C@@H]([C@H]2C1)C(=O)C=C1[C@@]2(C)C=C(C#N)C(=O)C(C)(C)C2CC[C@@]31C)C(O)=O
• Target: Virus Protease,Necroptosis,Nrf2,SARS-CoV
• Solubility: DMSO:16 mg/mL (32.54 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.14 mM)

Bioactivity

• In Vivo:
  Kidney sections from monkeys treated with Bardoxolone methyl displayed a reduction in megalin protein expression, despite unchanged mRNA expression levels across all studied groups. Densitometry confirmed this reduction, indicating that Bardoxolone methyl significantly lowers megalin protein levels in the monkey kidney, without affecting cubilin protein or mRNA expression. Moreover, creatinine clearance in these monkeys significantly changed from the baseline and compared to vehicle-treated monkeys on day 28. Following 28 days of Bardoxolone methyl treatment, urinary albumin-to-creatinine ratios (UACRs) notably increased compared to vehicle-treated animals, with UACRs decreasing by 53.3% in vehicle-treated and increasing by 27.9% in Bardoxolone methyl-treated monkeys. In a separate study, male C57BL/6J mice were given Bardoxolone methyl orally during high-fat diet (HFD) feeding (HFD/BARD), with comparisons to mice solely on a high-fat (HFD) or a low-fat diet (LFD) for 21 weeks. HFD mice showed a significant increase in F4/80 crown-like structures by 95% and interstitial macrophages by 98% compared to LFD mice, both of which were substantially mitigated in HFD/BARD mice, showing reductions of 50% and 32% respectively, in these markers of inflammation.
• In Vitro:
  Bardoxolone methyl is a novel synthetic triterpenoid and antioxidant inflammation modulator that potently induces Nrf2 and inhibits NF-κB and Janus-activated kinase/STAT signaling. Bardoxolone methyl has been shown to induce differentiation, inhibit proliferation, and induce apoptosis in cancer cell lines.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Bardoxolone, CDDO, Nrf2, Inhibitor, Keap1-Nrf2, inhibit, RTA 401, RTA401, RTA-401

Compound Identifiers

PubChem CID

24896136