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Opicapone
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Opicapone图片
CAS NO:923287-50-7
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
BIA 9-1067
产品介绍
Opicapone 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。

产品描述

Opicapone 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].

Cas No.

923287-50-7

分子式

C15H10Cl2N4O6

分子量

413.17

别名

BIA 9-1067

储存和溶解度

DMSO:100 mg/mL (242.03 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years