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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
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有货
概述
Tolcapone是一种有效和选择性的可逆硝基酚类儿茶酚-O-甲基转移酶(COMT)抑制剂，Ki为30nM。An inhibitor of peripheral and central catechol-O-methyltransferase.
Information
Tolcapone Tolcapone (Ro 40-7592) is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with K i of 30 nM.
In vitro
Tolcapone functions as a selective peripheral and central COMT inhibitor, exerting no effect on adrenergic, serotonergic, or cholinergic receptors or other enzymes involved in synthesis or catabolism of catecholamines. Tolcapone produces a concentration-dependent decrease in COMT activity in liver homogenates of developing (3 days-old) and adult (60 days-old) rats with Vmax, Km and IC50 of 5.3 nM/mg/h, 3.3 μM, 41 nM, and 2.9 nM/mg/h, 13.1 μM, 720 nM, respectively. Tolcapone produces a concentration-dependent decrease in COMT activity in kidney of developing (3 days-old) and adult (60 days-old) rats with Vmax, Km and IC50 of 2.6 nM/mg/h, 2.7 μM, 8 nM, and 3.5 nM/mg/h, 24 μM, 177 nM, respectively.
In vivo
Tolcapone orally administrated is able to crosses the blood-brain barrier. Acute administration of Tolcapone increases basal levels of L-DOPA and dihydroxyphenylacetic acid (DOPAC) and decreases basal homovanillic acid (HVA) levels, but does not affect basal dopamine levels. Tolcapone (30 mg/kg p.o.) combined with benserazide (15 mg/kg p.o.) and a low dose of L-dopa (10 mg/kg p.o.) almost completely blockes (for about 6 h) the formation of 3-O-methyldopa (3-OMD) in brain and plasma, producing a long-lasting increase of L-DOPA in plasma and a parallel marked increase of L-DOPA and dopamine in the brain. Tolcapone displays behavioural and neurochemical benefits on animals. Tolcapone (30 mg/kg p.o.) increases the effect of L-DOPA (plus benserazide) on locomotor activity, reserpine-induced hypothermia, and catalepsy induced by pimozide, haloperidol and fluphenazine. Tolcapone also increases locomotor hyperactivity induced by amphetamine or nomifensine, as well as stereotypy induced by amphetamine (but not apomorphine).
Cell Data
cell lines：
Concentrations：
Incubation Time：
Powder Purity:≥99%
规格
英文别名
Ro 40-7592 | Methanone, (3,4-dihydroxy-5-nitrophenyl)(4-methylphenyl)-
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Tolcapone
生化机理
托卡朋（Ro 40-7592）是一种选择性、强效、可逆的儿茶酚-O-甲基转移酶（COMT）抑制剂，其Ki值为 30 nM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
儿茶酚 O-甲基转移酶抑制剂
名称和识别符
EC号
694-343-9
分子类型
小分子
Isomeric SMILES
CC1=CC=C(C=C1)C(=O)C2=CC(=C(C(=C2)O)O)[N+](=O)[O-]
PubChem CID
分子量
273.24
高级数据
产品属性
| ALogP | 3.3 |
|---|
关联靶点（人）
TTR
Tclin
转甲状腺素蛋白(Transthyretin)
(4 活性数据)
COMT
Tclin
儿茶酚氧位甲基转移酶(Catechol O-methyltransferase)
(3 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro
熔点
145 °C
安全和危险性（GHS）
象形图
信号词
警告
危险声明
H400: 对水生生物毒性极大
预防措施声明
P273: 避免释放到环境中。
P501: 将内容物/容器送到批准的废物处理厂处理
P391: 收集溢出物
RTECS
PC4952500
Merck Index
9508
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
此产品的引用文献
溶液计算器
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