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分子生物学
IVD分子诊断
细胞培养与分析
蛋白研究
细胞因子
重组蛋白
抗体
高通量测序建库
病原检测UCF系列
生物医药
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抑制剂激活剂与常用试剂
仪器
耗材
Higenamine 去甲乌药碱
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已发表文献
产品介绍

Higenamine(去甲乌药碱)是中药乌头的关键成分,也是可从乌头毒草中分离得到的选择性LSD1抑制剂(IC50=1.47μM),兼具β2-AR激动剂和α1-肾上腺素受体拮抗剂活性,盐酸盐形式具有抗炎、抗菌及抗氧化能力,生物功能广泛且机制多样,可用于心力衰竭、癌症等多种疾病研究,其核心信息如下:作为β2-AR激动剂能保护心肌细胞,作为α1-肾上腺素受体拮抗剂可发挥降压效果,通过选择性激活β2-AR抵御心肌细胞凋亡和缺血/再灌注(I/R)损伤、降低小鼠I/R诱导的心肌梗死,还能通过ROS介导的PI3K/Akt信号通路减弱IL-1β引起的凋亡、保护脑细胞免受缺氧损伤,同时通过SMAD2/3途径促进骨质疏松症的骨形成,在MV4-11和MOLM-13细胞中(3-100μM,72小时)可通过抑制LSD1活性促进细胞分化,研究应用覆盖心力衰竭、癌症、炎症、心肾综合征、骨质疏松症等多个疾病领域。

产品性质
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存储条件
2~8℃避光保存,有效期3年。
COA
已发表文献

[1] Fang Y, Yang C, Teng D, Su S, Luo X, Liu Z, Liao G. Discovery of higenamine as a potent, selective and cellular active natural LSD1 inhibitor for MLL-rearranged leukemia therapy. Bioorg Chem. 2021 Apr;109:104723. doi: 10.1016/j.bioorg.2021.104723. Epub 2021 Feb 10. PMID: 33618250.[2]Ha YM, Kim MY, Park MK, Lee YS, Kim YM, Kim HJ, Lee JH, Chang KC. Higenamine reduces HMGB1 during hypoxia-induced brain injury by induction of heme oxygenase-1 through PI3K/Akt/Nrf-2 signal pathways. Apoptosis. 2012 May;17(5):463-74. doi: 10.1007/s10495-011-0688-8. PMID: 22183510.[3]Zhu X, Liu S, Cao Z, Yang L, Lu F, Li Y, Hu L, Bai X. Higenamine mitigates interleukin-1β-induced human nucleus pulposus cell apoptosis by ROS-mediated PI3K/Akt signaling. Mol Cell Biochem. 2021 Nov;476(11):3889-3897. doi: 10.1007/s11010-021-04197-z. Epub 2021 Jun 19. PMID: 34146182.[4]Dong H, Liu R, Zou K, Jin Z, Kang J, Zhang Y, Zhang X, Sun Z, Yu G, Huang N, Bretches M, Yang SY, Ning B. Higenamine Promotes Osteogenesis Via IQGAP1/SMAD4 Signaling Pathway and Prevents Age- and Estrogen-Dependent Bone Loss in Mice. J Bone Miner Res. 2023 May;38(5):775-791. doi: 10.1002/jbmr.4800. Epub 2023 Mar 29. PMID: 36907987.[5]Wu MP, Zhang YS, Zhou QM, Xiong J, Dong YR, Yan C. Higenamine protects ischemia/reperfusion induced cardiac injury and myocyte apoptosis through activation of β2-AR/PI3K/AKT signaling pathway. Pharmacol Res. 2016 Feb;104:115-23. doi: 10.1016/j.phrs.2015.12.032. Epub 2015 Dec 30. PMID: 26746354; PMCID: PMC4772856.[6]Deng T, Wei Z, Gael A, Deng X, Liu Y, Lai J, Hang L, Yan Q, Fu Q, Li Z. Higenamine Improves Cardiac and Renal Fibrosis in Rats With Cardiorenal Syndrome via ASK1 Signaling Pathway. J Cardiovasc Pharmacol. 2020 Jun;75(6):535-544. doi: 10.1097/FJC.0000000000000822. PMID: 32168151.

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