Tolcapone (Synonyms: 托卡朋; Ro 40-7592)

目录号: HY-17406 纯度: 99.91%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Tolcapone (Ro 40-7592) 是一种选择性，有效的，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。Tolcapone 还是一种 α-syn 和 Aβ42 寡聚和原纤维形成的有效抑制剂。Tolcapone 诱导氧化应激导致神经母细胞瘤细胞凋亡(apoptosis) 和抑制肿瘤生长。

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Tolcapone Chemical Structure

CAS No. : 134308-13-7

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥567	In-stock
5 mg	￥306	In-stock
10 mg	￥515	In-stock
50 mg	￥1234	In-stock
100 mg	￥1626	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Tolcapone:

MCE 顾客使用本产品发表的 2 篇科研文献

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生物活性
纯度 & 产品资料
参考文献

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^[1]. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis^[2]. Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in neuroblastoma^[3].

IC₅₀ & Target

COMT^[1]
α-syn and Aβ42 oligomerization, fibrillogenesis^[2]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BHK-21	CC₅₀	29.2 μM Compound: 22	Cytotoxicity against golden hamster BHK-21 cells incubated for 24 hrs by CCK-8 assay Cytotoxicity against golden hamster BHK-21 cells incubated for 24 hrs by CCK-8 assay	[PMID: 34458734]
HEK293	IC₅₀	< 1 nM Compound: 1	Inhibition of human MB-COMT expressed in HEK293 cells using dopamine as substrate and SAM as cofactor preincubated for 30 mins followed by substrate addition and measured after 40 mins by HTRF assay Inhibition of human MB-COMT expressed in HEK293 cells using dopamine as substrate and SAM as cofactor preincubated for 30 mins followed by substrate addition and measured after 40 mins by HTRF assay	[PMID: 32038769]
HeLa	CC₅₀	> 25 μM Compound: Tolcapone	Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Blue assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Blue assay	[PMID: 33851839]
HeLa	IC₅₀	50 μM Compound: Tolcapone	Inhibition of human KLF10 expressed in human HeLa cells assessed as reduction in transcriptional activity after 24 hrs by CACCC-responsive promoter driven TK-luciferase reporter gene assay Inhibition of human KLF10 expressed in human HeLa cells assessed as reduction in transcriptional activity after 24 hrs by CACCC-responsive promoter driven TK-luciferase reporter gene assay	[PMID: 25581017]
HT-29	EC₅₀	7.44 μM Compound: Tolcapone	Agonist activity at GPR35 in human HT-29 cells assessed as induction of whole cell dynamic mass redistribution after 50 mins by resonant waveguide grating biosensor analysis Agonist activity at GPR35 in human HT-29 cells assessed as induction of whole cell dynamic mass redistribution after 50 mins by resonant waveguide grating biosensor analysis	10.1039/C2MD20210G
U2OS	EC₅₀	49.2 μM Compound: Tolcapone	Agonist activity at GPR35 in human U2OS cells assessed as induction of beta-arrestin translocation after 5 hrs by beta-lactamase reporter gene assay Agonist activity at GPR35 in human U2OS cells assessed as induction of beta-arrestin translocation after 5 hrs by beta-lactamase reporter gene assay	10.1039/C2MD20210G

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^[3].
? Tolcapone (25, 50,75, 100 μM) treatment activates downstream apoptotic events in NB cells. Tolcapone induces caspase-mediated apoptosis in neuroblastoma^[3].

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

Cell Viability Assay^[3]

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^[3]

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^[3].

MCE 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 ^[3]
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 mm³ compared to control tumors of 1100±450 mm³.

Clinical Trial

分子量

273.24

Formula

C₁₄H₁₁NO₅

CAS 号

134308-13-7

性状

固体

颜色

Colorless to light yellow

中文名称

托卡朋

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (365.98 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

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

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 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

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.15 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (9.15 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（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。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.91%

选择批次：

Data Sheet (636 KB) SDS (459 KB)

COA (199 KB) HNMR (249 KB) LCMS (268 KB)

产品使用指南 (1538 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Tolcapone 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.6598 mL	18.2989 mL	36.5979 mL	91.4947 mL
	5 mM	0.7320 mL	3.6598 mL	7.3196 mL	18.2989 mL
	10 mM	0.3660 mL	1.8299 mL	3.6598 mL	9.1495 mL
	15 mM	0.2440 mL	1.2199 mL	2.4399 mL	6.0996 mL
	20 mM	0.1830 mL	0.9149 mL	1.8299 mL	4.5747 mL
	25 mM	0.1464 mL	0.7320 mL	1.4639 mL	3.6598 mL
	30 mM	0.1220 mL	0.6100 mL	1.2199 mL	3.0498 mL
	40 mM	0.0915 mL	0.4575 mL	0.9149 mL	2.2874 mL
	50 mM	0.0732 mL	0.3660 mL	0.7320 mL	1.8299 mL
	60 mM	0.0610 mL	0.3050 mL	0.6100 mL	1.5249 mL
	80 mM	0.0457 mL	0.2287 mL	0.4575 mL	1.1437 mL
	100 mM	0.0366 mL	0.1830 mL	0.3660 mL	0.9149 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

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沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Tolcapone (Synonyms: 托卡朋; Ro 40-7592)

Customer Review

Other Forms of Tolcapone:

MCE 顾客使用本产品发表的 2 篇科研文献