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• 产品描述： Entacapone (OR-611) 抑制儿茶酚-O-甲基转移酶(COMT)活性，IC50为151 nM。Entacapone 是一种 FTO demethylation 的抑制剂，IC50为3.5 μM，可用于代谢紊乱的研究

• 靶点： COMT:151 nM

• 体外研究： Entacapone在不同组织中抑制catechol-O-methyltransferase(COMT)的IC50值大体相似，包括肝脏，十二指肠, 肾脏和肺, 但是entacapone在这些组织中抑制效果比tolcapone更好。 Entacapone (< 100 μM)可以有效抑制α-syn和β-amyloid (Aβ) 齐聚反应和原纤维生成同时可以保护PC12细胞免受这两种蛋白聚集诱导的细胞外毒性

• 体内研究： Entacapone administration reduced body weight and lowered fasting blood glucose concentrations in diet-induced obese mice.

• 细胞实验： Cell lines: PC12 cells Concentrations: 5 μM Incubation Time: 72 h Method: Cells were treated with various concentrations of drug for 72 h.

• 动物实验： Animal Models: Male C57BL/6 mice Dosages: 600 mg/kg Administration: p.o.

• 参考文献：
  1. De Santi C, et al. Catechol-O-methyltransferase: variation in enzyme activity and inhibition by entacapone and tolcapone. Eur J Clin Pharmacol, 1998, 54(3), 215-219. 2. Di Giovanni S, et al. Entacapone and tolcapone, two catechol O-methyltransferase inhibitors, block fibril formation of alpha-synuclein and beta-amyloid and protect against amyloid-induced toxicity. J Biol Chem, 2010, 285(20), 14941-14954. 3. Jenner P, et al. Avoidance of dyskinesia: preclinical evidence for continuous dopaminergic stimulation. Neurology, 2004, 62(1 Suppl 1), S47-55. 4. Hamaue N, et al. Entacapone, a catechol-O-methyltransferase inhibitor, improves the motor activity and dopamine content of basal ganglia in a rat model of Parkinson's disease induced by Japanese encephalitis virus. Brain Res, 2010, 1309, 110-115. 5. Peng S, et al. Identification of entacapone as a chemical inhibitor of FTO mediating metabolic regulation through FOXO1. Sci Transl Med. 2019 Apr 17;11(488):eaa

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存条件： 2-8℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.276 ml	16.378 ml	32.756 ml
  5 mM	0.655 ml	3.276 ml	6.551 ml
  10 mM	0.328 ml	1.638 ml	3.276 ml
  50 mM	0.066 ml	0.328 ml	0.655 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *