Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Opicapone (BIA 9-1067) 是第三代儿茶酚-O-甲基转移酶 (COMT)抑制剂,能够降低细胞 ATP 含量,IC50=98 μM。它有用于帕金森病和运动波动的研究潜力。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 337 | 现货 | ||
2 mg | ¥ 486 | 现货 | ||
5 mg | ¥ 786 | 现货 | ||
10 mg | ¥ 1,180 | 现货 | ||
25 mg | ¥ 1,980 | 现货 | ||
50 mg | ¥ 2,760 | 现货 | ||
100 mg | ¥ 3,790 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 928 | 现货 |
产品描述 | Opicapone (BIA 9-1067) reduces the ATP content of the cells (IC50: 98 μM). Opicapone is an effective third-generation catechol-O-methyltransferase inhibitor for the research of Parkinson's disease and motor fluctuations. |
体外活性 | Opicapone decreases the mitochondrial membrane potential of the cells (IC50: 181 μM). Opicapone has a prolonged inhibitory effect on peripheral COMT, which extends the bioavailability of L-DOPA, without inducing toxicity. Incubation of human primary hepatocytes for 24 h with increasing concentrations of Ro 40-7592, OR-611 or Opicapone resulted in a concentration-dependent decrease in the mitochondrial membrane potential of the cells, evaluated by the ratio JC-1 aggregates over JC-1 monomer (ratio λex 544 λem 590 over λex 485 λem 538) [1]. |
体内活性 | Opicapone inhibited rat peripheral COMT with ED50 values below 1.4 mg kg(-1) up to 6 h post-administration.?The effect was sustained over the first 8 h and by 24 h COMT had not returned to control values.?A single administration of opicapone resulted in increased and sustained plasma levodopa levels with a concomitant reduction in 3-O-methyldopa from 2 h up to 24 h post-administration, while tolcapone produced significant effects only at 2 h post-administration.?The effects of opicapone on brain catecholamines after levodopa administration were sustained up to 24 h post-administration.?Opicapone was also the least potent compound in decreasing both the mitochondrial membrane potential and the ATP content in human primary hepatocytes after a 24 h incubation period[1]. |
别名 | BIA 9-1067 |
分子量 | 413.17 |
分子式 | C15H10Cl2N4O6 |
CAS No. | 923287-50-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (242.03 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4203 mL | 12.1016 mL | 24.2031 mL | 60.5078 mL |
5 mM | 0.4841 mL | 2.4203 mL | 4.8406 mL | 12.1016 mL | |
10 mM | 0.242 mL | 1.2102 mL | 2.4203 mL | 6.0508 mL | |
20 mM | 0.121 mL | 0.6051 mL | 1.2102 mL | 3.0254 mL | |
50 mM | 0.0484 mL | 0.242 mL | 0.4841 mL | 1.2102 mL | |
100 mM | 0.0242 mL | 0.121 mL | 0.242 mL | 0.6051 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Opicapone 923287-50-7 Metabolism Transferase BIA 9-1067 Inhibitor inhibit COMT inhibitor