Micheliolide
A sesquiterpene lactone with diverse biological activities
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包装价格促销价数量
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5mg￥1525.001220.00- +
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10mg￥2375.001900.00- +
- 货号: ajce57454
- CAS: 68370-47-8
- 别名: 木香内酯
- 分子式: C15H20O3
- 分子量: 248.32
- 纯度: ＞98%
- 溶解度: DMSO: 100 mg/mL (402.71 mM)
- 储存: Store at -20°C
- 库存: 现货
Background
Micheliolide is a sesquiterpene lactone and derivative of parthenolide that has been found in M. champaca and has diverse biological activities.1,2,3,4 It is an irreversible activator of the pyruvate kinase M2 isoform (PKM2; EC50 = 6 nM) that decreases viability of HL-60 cells when used at concentrations ranging from 5 to 20 ?M.1 Micheliolide (5-10 ?M) reduces M. tuberculosis-induced secretion of IL-1β and TNF-α, expression of Cox2, and production of nitric oxide (NO) in RAW 264.7 cells.2 It also inhibits M. tuberculosis-induced NOD-, LRR-, and pyrin domain-containing protein 3 (NLRP3) inflammasome activation in RAW 264.7 cells. Micheliolide (30 mg/kg) decreases the severity of collagen-induced arthritis (CIA) in a mouse model of rheumatoid arthritis.3 It also increases hepatic protein levels of PPARγ and reduces hepatic inflammation and steatosis in db/db mice.4
1.Li, J., Li, S., Guo, J., et al.Natural product micheliolide (MCL) irreversibly activates pyruvate kinase M2 and suppresses leukemiaJ. Med. Chem.61(9)4155-4164(2018) 2.Zhang, Q., Jiang, X., He, W., et al.MCL plays an anti-inflammatory role in Mycobacterium tuberculosis-induced immune response by inhibiting NF-κB and NLRP3 inflammasome activationMediators Inflamm.2432904(2017) 3.Xu, H., Wang, J., Wang, C., et al.Therapeutic effects of micheliolide on a murine model of rheumatoid arthritisMol. Med. Rep.11(1)489-493(2015) 4.Zhong, J., Gong, W., Chen, J., et al.Micheliolide alleviates hepatic steatosis in db/db mice by inhibiting inflammation and promoting autophagy via PPAR-γ-mediated NF-кB and AMPK/mTOR signalingInt. Immunopharmacol.59197-208(2018)
