CAS NO: | 218600-44-3 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Bardoxolone is a novel nuclear regulator factor (Nrf-2) activator. | ||||||||||||||||
IC50& Target | Nrf-2[1] | ||||||||||||||||
体外研究 (In Vitro) | 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[2]. | ||||||||||||||||
体内研究 (In Vivo) | 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[3]. 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[4]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 491.66 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C31H41NO4 | ||||||||||||||||
CAS 号 | 218600-44-3 | ||||||||||||||||
中文名称 | 巴多索隆 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(203.39 mM;Need ultrasonic) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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