218600-44-3
Chemical Structure
Bardoxolone
Synonym(s): CDDO; RTA 401
- CAS 番号: 218600-44-3
- Formula:C31H41NO4
- Molecular Weight:491.66
IUPAC Name: (4aS,6aR,6bS,8aR,12aS,14aR,14bS)-11-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,3,4,5,6,6a,6b,7,8,8a,9,10,12a,14,14a,14b-hexadecahydropicene-4a(2H)-carboxylic acid
InChIKey: TXGZJQLMVSIZEI-UQMAOPSPSA-N
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
Biological Activity: Bardoxolone (CDDO; RTA 401) is a Nrf2 activator. Bardoxolone shows anti-SARS-CoV-2 3CLpro with IC50 of 27.99 μM. Bardoxolone activates the Nrf2 pathway and inhibits the NF-κB pathway. Bardoxolone can induce cells differentiation, apoptosis and shows antiproliferative activity against cancer cells. Bardoxolone can increase ROS and decrease intracellular GSH levels. Bardoxolone inhibits Z-VAD-FMK (HY-16658B)-induced necroptosis. Bardoxolone can be used for the research of cancer, inflammation and infection, such as SARS-CoV infection and glioblastoma[1][2][3].
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Bardoxolone | 99.50% | Bardoxolone (CDDO; RTA 401) is a Nrf2 activator. Bardoxolone shows anti-SARS-CoV-2 3CLpro with IC50 of 27.99 μM. Bardoxolone activates the Nrf2 pathway and inhibits the NF-κB pathway. Bardoxolone can induce cells differentiation, apoptosis and shows antiproliferative activity against cancer cells. Bardoxolone can increase ROS and decrease intracellular GSH levels. Bardoxolone inhibits Z-VAD-FMK (HY-16658B)-induced necroptosis. Bardoxolone can be used for the research of cancer, inflammation and infection, such as SARS-CoV infection and glioblastoma. | ||||||||||||||||||||
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Bardoxolone (Standard) | ≥98% | Bardoxolone (Standard) is the analytical standard of Bardoxolone (HY-14909). This product is intended for research and analytical applications. Bardoxolone 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. | ||||||||||||||||||||
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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]. Borella R, et al. Synthesis and Anticancer Activity of CDDO and CDDO-Me, Two Derivatives of Natural Triterpenoids. Molecules. 2019;24(22):4097. Published 2019 Nov 13. [Content Brief]
- [3]. Wang Y, et al. Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors. Eur J Med Chem. 2021;212:113030. [Content Brief]
