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Biochanin A
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Biochanin A
CAS No. : 491-80-5
MCE 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
In Vitro: Biochanin A inhibits the hydrolysis of 0.5 ?M AEA by mouse, rat and human FAAH with IC50 s of 1.8, 1.4 and 2.4 ?M respectively. FAAH is inhibited by Biochanin A with a pIC50 value of 6.21±0.02, corresponding to an IC50 value of 0.62 ?M. 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 ?M [3H]AEA with assay conditions giving these higher utilization rates, the activity is still inhibited by Biochanin A, Genistein, Formotin and Daidzein in the low micromolar range (IC50s of 6.0, 8.4, 12 and 30 ?M, respectively).
In Vivo: Biochanin A is tested at doses of 30, 100 and 300 ?g. 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 ?g i.pl.) and Biochanin A (100 ?g 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 ?g 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.).
相关产品:Natural Product Library Plus | Bioactive Compound Library Plus | Metabolism/Protease Compound Library | Neuronal Signaling Compound Library | Natural Product Library | Anti-Cancer Compound Library | Autophagy Compound Library | Medicine Food Homology Compound Library | Traditional Chinese Medicine Monomer Library | Flavonoids Library | Carprofen | PF-3845 | FAAH-IN-2 | JZL195 | LY2183240 | 1-Monomyristin | N-Benzyloleamide | N-Benzylpalmitamide | SA 47 | FAAH inhibitor 1 | JNJ-1661010 | N-(3-Methoxybenzyl)Palmitamide | N-?Benzyllinolenamide | SA57 | Acetylhydrolase-IN-1 | SA72
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