2-氰基-3,12-二氧代齐墩果-1,9-二烯-28-酸
中文名称 | 2-氰基-3,12-二氧代齐墩果-1,9-二烯-28-酸 |
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中文同义词 | 2-氰基-3,12-二氧代齐墩果-1,9-二烯-28-酸;巴多索隆;齐墩果烷三萜化合物;NRF-2激活剂(BARDOXOLONE);2-氰基-3,12-二氧代齐墩果-1,9-二烯-28-酸, 一种新型核调节因子 (NRF-2)激活剂;(4AS,6AR,6BS,8AR,12AS,14AR,14BS)-11-氰基-2,2,6A,6B,9,9,12A-七甲基-10,14-二氧代-1,3,4,5,6,6A,6B,7,8,8A,9,10,12A,14,14A,14B-十六氢蒎烯-4A(2H)-羧酸;BARDOXOLONE,诱导剂;RTA 401|||齐墩果烷三萜化合物|||CDDO |
英文名称 | Bardoxolone |
英文同义词 | 2-Cyano-3,12-dioxooleana-1,9-dien-28-oic acid;CDDO(Bardoxolone);BARDOXOLONE;CDDO;RTA 401;Oleana-1,9(11)-dien-28-oic acid, 2-cyano-3,12-dioxo-;Bardoxolone;CDDO;RTA 401;2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid |
CAS号 | 218600-44-3 |
分子式 | C31H41NO4 |
分子量 | 491.66 |
EINECS号 | |
相关类别 | 信号转导通路激酶抑制剂;细胞凋亡;细胞生物学试剂;抑制剂;医药原料药 |
Mol文件 | 218600-44-3.mol |
结构式 |
2-氰基-3,12-二氧代齐墩果-1,9-二烯-28-酸 性质
熔点 | 180-182 °C |
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沸点 | 632.9±55.0 °C(Predicted) |
密度 | 1.18 |
储存条件 | Sealed in dry,Store in freezer, under -20°C |
溶解度 | DMSO 中≥49.2 mg/mL;不溶于水;温和加热和超声波下,乙醇中≥2.682 mg/mL |
形态 | 固体 |
酸度系数(pKa) | 4.52±0.70(Predicted) |
颜色 | 白色至黄色 |
Target | Value |
Nrf2
() |
Bardoxolone methyl, a novel synthetic triterpenoid and antioxidant inflammation modulator, 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.
Kidney sections from Bardoxolone methyl-treated monkeys demonstrates decreased megalin protein expression despite similar mRNA expression across groups. The visualized decrease in megalin protein expression is confirmed by densitometry analyses, which demonstrated that Bardoxolone methyl administration significantly decreased megalin protein expression in the monkey kidney. Bardoxolone methyl administration does not affect the protein expression of cubilin in the kidney or the mRNA expression of cubilin in the kidney. The creatinine clearance in monkeys administered Bardoxolone methyl significantly differed from that at baseline and in vehicle-treated animals on day 28. After 28 days of Bardoxolone methyl administration, urinary albumin-to-creatinine ratios (UACRs), determined from the 24-hour urine collections, are significantly increased compared with those in animals receiving vehicle. Of note, UACRs decreases 53.3% in vehicle-treated animals and increased 27.9% in Bardoxolone methyl-treated monkeys. Male C57BL/6J mice are administered oral BARD during HFD feeding (HFD/BARD), only fed a high-fat diet (HFD), or fed low-fat diet (LFD) for 21 weeks. Compared with LFD mice, HFD mice have a marked increase in the number of F4/80 crown-like structures (+95%; p<0.001), which is effectively prevented by BARD (−50%; p<0.01). Similarly, the number of F4/80 interstitial macrophages is significantly higher in HFD mice by 98% (p<0.001) compared with LFD mice and by 32% (p<0.01) compared with HFD/BARD mice.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/04/30 | S6647 | 2-氰基-3,12-二氧代齐墩果-1,9-二烯-28-酸 Bardoxolone | 218600-44-3 | 5mg | 970.53元 |
2024/04/30 | S6647 | 2-氰基-3,12-二氧代齐墩果-1,9-二烯-28-酸 Bardoxolone | 218600-44-3 | 25mg | 2970.62元 |