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CAS No. : 491-80-5
MCE 国际站:Biochanin A
产品活性:Biochanin A 是一种天然存在的脂肪酸酰胺水解酶 (FAAH) 抑制剂,抑制FAAH,作用于小鼠,大鼠,人 FAAH,IC50 分别为 1.8,1.4 和 2.4 μM。
研究领域:Metabolic Enzyme/Protease | Neuronal Signaling | Autophagy
作用靶点:FAAH | Autophagy | Endogenous Metabolite
结构分类:黄酮类 | 异黄酮 | 酚类 | 多酚类 | 结构分类
来源:植物 | 豆科 | 红车轴草
In Vitro: Biochanin A inhibits the hydrolysis of 0.5 μM AEA by mouse, rat and human FAAH with IC50 s of 1.8, 1.4 and 2.4 μM respectively. FAAH is inhibited by Biochanin A with a pIC50 value of 6.21±0.02, corresponding to an IC50 value of 0.62 μM. Biochanin A produces significant inhibition of the URB597-sensitive tritium retention at high nanomolar-low micromolar concentrations. Experiments are run with human FAAH and 0.5 μM [3H]AEA with assay conditions giving these higher utilization rates, the activity is still inhibited by Biochanin A, Genistein, Formononetin and Daidzein in the low micromolar range (IC50s of 6.0, 8.4, 12 and 30 μM, respectively).
In Vivo: Biochanin A is tested at doses of 30, 100 and 300 μg. The highest dose also reduced formalin-induced ERK phosphorylation in a manner antagonized by AM251. Thus, Biochanin A behaved like URB597 after local administration to the paw. In anaesthetized mice, URB597 (30 μg i.pl.) and Biochanin A (100 μg i.pl.) both inhibit the spinal phosphorylation of extracellular signal-regulated kinase produced by the intraplantar injection of formalin. The effects of both compounds are significantly reduced by the CB1 receptor antagonist/inverse agonist AM251 (30 μg i.pl.). Biochanin A (15 mg/k i.v.) does not increase brain AEA concentrations, but produces a modest potentiation of the effects of 10 mg/kg i.v. AEA in the tetrad test. Biochanin A (15 mg/kg i.v.) is without effects on its own, but significantly potentiates the effects of AEA (10 mg/kg i.v.).
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货号: HY-14595
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