MedChemExpress -Model Bardoxolone -218600-44-3

FromMedChemExpress LLC (MCE)

Bardoxolone (RTA 401; CDDO) is a novel nuclear regulatory factor (NRf-2) activator. Bardoxolone is a potent necroptosis inhibitor that inhibits Z-VAD-FMK-induced necroptosis. Bardoxolone methyl enhances the antioxidant system, modulates inflammatory cytokines and inhibits apoptosis in rat kidney, demonstrating inhibition on APAP-induced acute kidney injury (AKI) and analgesic effect. Additionally, Bardoxolone methyl decreases Paclitaxel (PAC) (HY-B0015)-induced mitochondrial damage in neuronal cells. Bardoxolone methyl is promising for the research of chemotherapy-induced neuropathic pain and chronic kidney disease[1][2][3][4].

Bardoxolone

MCE China：Bardoxolone

Brand：MedChemExpress (MCE)

Cat. No.HY-14909

CAS：218600-44-3

Synonyms：CDDO; RTA 401

Purity：98.57%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Bardoxolone (RTA 401; CDDO) is a novel nuclear regulatory factor (NRf-2) activator. Bardoxolone is a potent necroptosis inhibitor that inhibits Z-VAD-FMK-induced necroptosis. Bardoxolone methyl enhances the antioxidant system, modulates inflammatory cytokines and inhibits apoptosis in rat kidney, demonstrating inhibition on APAP-induced acute kidney injury (AKI) and analgesic effect. Additionally, Bardoxolone methyl decreases Paclitaxel (PAC) (HY-B0015)-induced mitochondrial damage in neuronal cells. Bardoxolone methyl is promising for the research of chemotherapy-induced neuropathic pain and chronic kidney disease.

In Vitro：Bardoxolone methyl (5, 10 mg/kg) significantly decreases in levels of renal KIM-1, NGAL, TNF-α, TOS, OSI and improves deterioration in glomeruli and tubules similarly to NAC (HY-B0215) in rat kidney homogenates[3]. Bardoxolone methyl (0.3 and 1 μM, 28 h) decreases PAC-induced mitochondrial damage in the dorsal root ganglia (DRG) neuronal cell lines and increases pNRf2 intensity in the PAC-treated DRG cells[4].

In Vivo：Bardoxolone methyl(5, 10 mg/kg) decreased the percentage of caspase-3 immunopositive cells in a dose-dependent manner in rat kidney [3]. Bardoxolone methyl (0-10 mg/kg, i.p., a single dose) results in analgesia but not sedation in rats[4]. Bardoxolone methyl [10 mg/kg, twice-daily on day 21 after the first PAC (HY-B0015) injection] decreases PAC-induced levels of pNFκB and MCP-1 by increasing pNRf2 and HO-1 in rat DRG[4].

IC50 & Target：Nrf-2[1] Cellular Effect Cell Line Type Value Description References

References：

[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. [Content Brief]

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

[3]. Yasemin Teksen, et al. Bardoxolone methyl attenuates acetaminophen-induced acute kidney injury by suppressing oxidative stress, inflammation and apoptosis[J]. 2024 May 29;31(5):372–379

[4]. Kim HK, et al. Bardoxolone Methyl Ameliorates Chemotherapy-Induced Neuropathic Pain by Activation of Phosphorylated Nuclear Factor Erythroid 2-Related Factor 2 in the Dorsal Root Ganglia. Anesth Analg. 2024 Mar 1;138(3):664-675. [Content Brief]

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