化合物Opicapone T16398

Product Introduction
Bioactivity


英文名: Opicapone

描述: 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。

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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 100 mg/mL (242.03 mM)


关键字: Inhibitor | inhibit | COMT | Opicapone

相关产品: L-778123 hydrochloride | AMP-Deoxynojirimycin | Pradigastat | Alendronate sodium hydrate | Nialamide | FTI-277 hydrochloride | Rosmarinic acid | CP-609754 | Serotonin | Lonafarnib

相关库: Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | ReFRAME Related Library | Anti-Parkinson's Disease Compound Library | Clinical Compound Library | Anti-Metabolism Disease Compound Library | Bioactive Compounds Library Max | Human Metabolite Library | Inhibitor Library | EMA Approved Drug Library

化合物Opicapone T16398信息由TargetMol中国为您提供，如您想了解更多关于化合物Opicapone T16398报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途