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
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;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;NRF-2激活剂(BARDOXOLONE)
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:
细胞生物学试剂;信号转导通路激酶抑制剂;细胞凋亡;抑制剂
Mol文件:
218600-44-3.mol
熔点
180-182 °C
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
酸度系数(pKa)
4.52±0.70(Predicted)
生物活性
Bardoxolone (CDDO, RTA 401)通过从KEAP1释放Nrf2起作用，是Nrf2的激活剂，可以诱导癌细胞凋亡。
靶点
Target Value
Nrf2
()
Target
Value
Nrf2
()
体外研究
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.
体内研究
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.
