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Bardoxolone,诱导剂

规格或纯度: ≥98%
有货

库存信息

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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
B125862-25mg
 25mg 现货 Stock Image
B125862-100mg
 100mg 期货 Stock Image
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kelch like ECH-associated protein 1 Peroxisome proliferator-activated receptor-γ Agonist
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基本描述

规格或纯度 ≥98%
英文名称 Bardoxolone
别名 CDDO;RTA 401
英文别名 CDDO;RTA 401;RTA401;RTA-401;2-Cyano-3,12-dioxooleana-1,9-dien-28-oic acid
生化机理

Bardoxolone methyl, previously known as RTA 402, is the lead molecule in Reata's portfolio of Antioxidant Inflammation Modulators (AIMs). The AIMs are potent inducers of the transcription factor Nrf2, an important biological target that controls the production of many of the body's antioxidant and detoxification enzymes. Because oxidative stress and inflammation occur throμghout the course of chronic kidney disease (CKD) and are known to contribute to loss of kidney function, agents that activate the Nrf2 pathway in patients with CKD may provide a novel method for preserving or improving kidney function. Bardoxolone methyl is currently being investigated as a potential oral once-a-day treatment for CKD.

储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 卖完停产，不再备货
产品介绍

Bardoxolone(RTA 402)是抗氧化炎症调节剂（AIM）的先导化合物，此类AIM是转录因子Nrf2诱导剂。

Bardoxolone(RTA 402) is the lead molecule in Reata's portfolio of Antioxidant Inflammation Modulators (AIMs). The AIMs are potent inducers of the transcription factor Nrf2.

名称和标识符

IUPAC Name (4aS,6aR,6bS,8aR,12aS,14aR,14bS)-11-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,3,4,5,6,7,8,8a,14a,14b-decahydropicene-4a-carboxylic acid
INCHI InChI=1S/C31H41NO4/c1-26(2)10-12-31(25(35)36)13-11-30(7)23(19(31)16-26)20(33)14-22-28(5)15-18(17-32)24(34)27(3,4)21(28)8-9-29(22,30)6/h14-15,19,21,23H,8-13,16H2,1-7H3,(H,35,36)/t19-,21-,23-,28-,29+,30+,31-/m0/s1
InChi Key TXGZJQLMVSIZEI-UQMAOPSPSA-N
Canonical SMILES CC1(CCC2(CCC3(C(C2C1)C(=O)C=C4C3(CCC5C4(C=C(C(=O)C5(C)C)C#N)C)C)C)C(=O)O)C
PubChem CID 400010
分子量 491.66

化学和物理性质

溶解性 DMSO

关联配体

Ligand ID 2717
名称 bardoxolone
别名 CDDO
类别 Synthetic organic
学名 (4aS,6aR,6bS,8aR,12aS,14aR,14bS)-11-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,3,4,5,6,7,8,8a,14a,14b-decahydropicene-4a-carboxylic acid
生物活性评价 The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价 Bardoxolone was a Phase 3 NF-κB signaling inhibitor . Although the recommended INN for this compound is bardoxolone, it is administered as bardoxolone methyl which has ChEMBL ID CHEMBL1762621. Bardoxolone can be described as a KEAP1 antagonist, as it antigonises KEAP1 interaction with the Nrf2 transription factor . As this action releases Nrf2 from the inhibitory effect of the protein-protein interaction, it can also be described as a functional Nrf2 activator.

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参考文献

1. Dinkova-Kostova AT, Liby KT, Stephenson KK, Holtzclaw WD, Gao X, Suh N, Williams C, Risingsong R, Honda T, Gribble GW et al..  (2005)  Extremely potent triterpenoid inducers of the phase 2 response: correlations of protection against oxidant and inflammatory stress..  Proc Natl Acad Sci USA,  102  (12):  (4584-9).  [PMID:15767573]
2. Rojas-Rivera J, Ortiz A, Egido J.  (2012)  Antioxidants in kidney diseases: the impact of bardoxolone methyl..  Int J Nephrol,  2012  (13):  (321714).  [PMID:22701794]
3. Wu J, Liu X, Fan J, Chen W, Wang J, Zeng Y, Feng X, Yu X, Yang X.  (2014)  Bardoxolone methyl (BARD) ameliorates aristolochic acid (AA)-induced acute kidney injury through Nrf2 pathway..  Toxicology,  318  (13):  (22-31).  [PMID:24530882]
4. Cleasby A, Yon J, Day PJ, Richardson C, Tickle IJ, Williams PA, Callahan JF, Carr R, Concha N, Kerns JK et al..  (2014)  Structure of the BTB domain of Keap1 and its interaction with the triterpenoid antagonist CDDO..  PLoS ONE,  9  (6):  (e98896).  [PMID:24896564]
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