Tolcapone|134308-13-7|(托卡朋; Ro 40-7592)-陌孚医药/Medlife

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Tolcapone (Synonyms: 托卡朋; Ro 40-7592)

目录号: PC12527 纯度: ≥98%

CAS No. :134308-13-7

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PC12527-50mg	50mg	¥1528.00	请登录
PC12527-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥700.00	请登录

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中文名称

Tolcapone

中文别名

托卡朋;(3,4-二羟基-5-硝基苯基)-(4-甲基苯基)甲酮;2-氨基-5-(4-溴苯基)-1,3,4-噻二唑;托卡朋 USP标准品;甲达沙星;甲磺酸达氟沙星;甲磺酸丹诺沙星;3,4-二羟基-4'-甲基-5-硝基苯甲酮

英文名称

Tolcapone

英文别名

Tolcapone;(3,4-dihydroxy-5-nitrophenyl)-(4-methylphenyl)methanone;Methanone, (3,4-dihydroxy-5-nitrophenyl)(4-methylphenyl)-;Ro 40-7592;(3,4-Dihydroxy-5-nitrophenyl)(4-methylphenyl)methanone;[14C]-Tolcapone;1-(3,4-dihydroxy-5-nitrophenyl)-1-(4-methylphenyl)methanone;3,4-Dihydroxy-4'-methyl-5-nitrobenzophenone;4'-methyl-3,4-dihydroxy-5-nitro-benzophenone;Methanone,(3,4-dihydroxy-5-nitrophenyl)(4-methylphenyl);Tasmar;Tasmar (TN);UNII-CIF6334OLY;3,4-Dihydroxy-4′-methyl-5-nitrobenzophenone;(3,4-dihydroxy-5-nitrophenyl)(p-tolyl)methanone;Talcapone;CIF6334OLY;C14H11NO5;DSSTox_CID_3685;DSSTox_RID_77146;DSSTox_GSID_23685;Tolcapon

Cas No.

134308-13-7

分子式

C₁₄H₁₁NO₅

分子量

273.24

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Tolcapone (Ro 40-7592) is a selective, orally active and powerful mixed (peripheral and central) COMT inhibitor with an IC₅₀ of 773?nM in the liver. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis. Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in neuroblastoma.

性状

Solid

IC50 & Target[1][2]

COMT
α-syn and Aβ42 oligomerization, fibrillogenesis

体外研究(In Vitro)

Tolcapone is cytotoxic to neuroblastoma (NB) cells with IC₅₀ values ranging from 32.27 μM for SMS-KCNR cells to 219.8 μM for MGT9-102-08 primary cells.
Tolcapone (25, 50,75, 100 μM) treatment activates downstream apoptotic events in NB cells. Tolcapone induces caspase-mediated apoptosis in neuroblastoma.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	BE(2)-C, SMS-KCNR, CHLA-90, SH-SY5Y, MGT-015-08 and MGT9-102-08
Concentration:	1.5625~400 μM
Incubation Time:	48 hours
Result:	IC₅₀s of 32.27, 72.31, 80.29, 109.4, 174.6, 219.8 μM for SMS-KCNR, SH-SY5Y, BE(2)-C, CHLA-90, MGT-015-08 and MGT9-102-08, respectively.

Cell Viability Assay

Cell Line:	NB cell lines: BE(2)-C, SMS-KCNR, CHLA-90, SH-SY5Y, MGT-015-08 and MGT9-102-08
Concentration:	25, 50, 75, 100 μM
Incubation Time:
Result:	A dose-dependent increase in cleaved caspase-3 and cleaved PARP protein in all six NB cell lines and a subsequent decrease in whole caspase-3 and whole PARP protein.

体内研究(In Vivo)

Tolcapone (125 mg/kg; orally) inhibits tumor growth and prolongs survival in vivo. There are no adverse events or differences in weight or behavior noted in the mice.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	4-week-old female nude mice (nu/nu) bearing SMS‐KCNR xenograft models
Dosage:	125 mg/kg
Administration:	Treated orally every 24 h for 35 days
Result:	Decreased tumor volume compared to control. Resulted in a smaller average tumor of 490±310 mm compared to control tumors of 1100±450 mm.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Catechol-O-methyltransferase: variation in enzyme activity and inhibition by entacapone and tolcapone. C De Santi, et al. Eur J Clin Pharmacol. 1998 May;54(3):215-9. [Information]

[2]. Saviana Di Giovanni, et al. Entacapone and tolcapone, two catechol O-methyltransferase inhibitors, block fibril formation of alpha-synuclein and beta-amyloid and protect against amyloid-induced toxicity. J Biol Chem. 2010 May 14;285(20):14941-14954. [Information]

[3]. Tyler Maser,et al. Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in Neuroblastoma.Cancer Med. 2017 Jun;6(6):1341-1352. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (365.98 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.6598 mL	18.2989 mL	36.5979 mL
5 mM	0.7320 mL	3.6598 mL	7.3196 mL
10 mM	0.3660 mL	1.8299 mL	3.6598 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (9.15 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (9.15 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (9.15 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (9.15 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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