Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 27.3 mg/mL (100 mM)
DMSO: 27.3 mg/mL (100 mM)
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 |
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。
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