首页 工具
登录
购物车
Tolcapone

Tolcapone

产品编号 T6708   CAS 134308-13-7
别名: Tasmar, Ro 40-7592, 托卡朋

Tolcapone (Ro 40-7592) 是一种选择性,具有口服活性的外周和中枢COMT 抑制剂,在肝脏中对 COMT 的IC50为 773 nM。它还是一种 α-syn 和 Aβ42 寡聚和原纤维形成的有效抑制剂,可诱导氧化应激导致神经母细胞瘤细胞凋亡和抑制肿瘤生长。

TargetMol的所有产品和服务仅用于科学研究,不能被用于人体,我们也不向个人提供产品和服务。
Tolcapone Chemical Structure
Tolcapone, CAS 134308-13-7
规格 价格/CNY 货期 数量
5 mg ¥ 245 现货
10 mg ¥ 426 现货
25 mg ¥ 688 现货
50 mg ¥ 987 现货
100 mg ¥ 1,350 现货
200 mg ¥ 1,960 现货
500 mg ¥ 3,380 现货
1 mL * 10 mM (in DMSO) ¥ 385 现货
其他形式的 Tolcapone:
产品目录号及名称: Tolcapone (T6708)
点击图片重新获取验证码
选择批次  
纯度: 99.89%
纯度: 99.49%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Tolcapone (Ro 40-7592) is a catechol-O-methyltransferase inhibitor used in the therapy of Parkinson disease as adjunctive therapy in combination with levodopa and carbidopa.
靶点活性 COMT:30 nM(Ki)
体外活性 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. [1] 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. [2]
体内活性 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. [3] 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. [4] 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). [5]
激酶实验 Enzyme assay and binding assay: Protein kinase C is assayed in a reaction mixture (0.25 mL) containing 5 μmol of Tris/HCl, pH 7.5, 2.5 μmol of magnesium acetate, 50 μg of histone II S, 20 μg of phosphatidylserine, 0.88 μg of diolein, 125 nmol of CaCl2, 1.25 nmol of [γ-32]ATP (5-10 × 104 cpm/nmol) and 5 μg of partially purified enzyme. The binding of [3H]PDBu to protein kinase C is determined: Reaction mixture (200 μL contained 4 μmo1 of Tris/malate, pH 6.8, 20 μmol of KCl, 30 nmol of CaC12, 20 μg of phosphatidylserine, 5 μg of partially purified protein kinase C, 0.5% (final concentration) of DMSO,10 pmol of [3H]PDBu (l-3 × 104 cpm/pmol) and 10 μL of various amounts of Staurosporine.
别名 Tasmar, Ro 40-7592, 托卡朋
分子量 273.24
分子式 C14H11NO5
CAS No. 134308-13-7

存储

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

溶解度

Ethanol: 27.3 mg/mL (100 mM)

DMSO: 27.3 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 3.6598 mL 18.2989 mL 36.5979 mL 91.4947 mL
5 mM 0.732 mL 3.6598 mL 7.3196 mL 18.2989 mL
10 mM 0.366 mL 1.8299 mL 3.6598 mL 9.1495 mL
20 mM 0.183 mL 0.9149 mL 1.8299 mL 4.5747 mL
50 mM 0.0732 mL 0.366 mL 0.732 mL 1.8299 mL
100 mM 0.0366 mL 0.183 mL 0.366 mL 0.9149 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
=
X
X
X
=
X
=
/
g/mol

输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Zürcher G, et al. Adv Neurol, 1990, 53:497-50 2. Vieira-Coelho MA, et al. Br J Pharmacol, 1996, 117(3), 516-520. 3. Brannan T, et al. Neurology, 1992, 42(3 Pt 1), 683-685. 4. Zürcher G, et al. J Neural Transm Suppl, 1990, 32, 375-38 5. Maj J, et al. J Neural Transm Park Dis Dement Sect, 1990, 2(2), 101-112. 6. Qiu M, Li Z, Chen Y, et al. Tolcapone Potently Inhibits Seminal Amyloid Fibrils Formation and Blocks Entry of Ebola Pseudoviruses. Frontiers in Microbiology. 2020, 11: 504.

文献引用

1. Qiu M, Li Z, Chen Y, et al. Tolcapone Potently Inhibits Seminal Amyloid Fibrils Formation and Blocks Entry of Ebola Pseudoviruses. Frontiers in Microbiology. 2020, 11: 504
Geniposide γ-Secretase-IN-1 2-O-Acetyl-20-hydroxyecdysone ALZ-801 BMS 433796 Schisandrone Anatabine Silybin B

相关化合物库

该产品包含在如下化合物库中:
神经退行性疾病化合物库 抗癌药物库 抗癌临床化合物库 抗癌上市药物库 抗癌活性化合物库 表型筛选靶点鉴定库 抗代谢疾病化合物库 FDA上市及药典收录分子库 已知活性化合物库 药物功能重定位化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

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。

Keywords

Tolcapone 134308-13-7 Apoptosis Metabolism Neuroscience Beta Amyloid Transferase central COMT Peripheral methyltransferase Tasmar Ro 40-7592 inhibit stress Abeta Inhibitor oxidative Neuroblastoma Amyloid-β 托卡朋 β-amyloid peptide inhibitor

 

陶术
生物
TargetMol®中国区唯一合作伙伴
点击进入陶术生物官网陶术生物
联系我们
400-820-0310

上海市静安区江场三路238号8楼