Ro 41-0960 - CAS:125628-97-9

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Ro 41-0960

目录号 : KCM10853 CAS No. : 125628-97-9 纯度 : ≥98%

Data Sheet SDS 产品使用指南

Ro 41-0960 is a catechol-O-methyltransferase (COMT) inhibitor. It prevents dopaminergic neuron loss induced by L-DOPA in primary rat rostral mesencephalic tegmentum cultures (EC = 0.1 µM). Ro 41-0960 (30 mg/kg) potentiates L-DOPA and carbidopa-induced reversal of reserpine-induced akinesias in rats and reserpine-induced catalepsy and hypothermia in mice. It reduces striatal 3-methyl-DOPA levels and increases striatal dopamine and 3,4-dihydroxyphenylacetic acid (DOPAC;) levels in rats. Ro 41-0960 (150 mg/kg) also reduces fibroid volume in the Eker rat model of uterine fibroids.

规格	价格	是否有货	数量
10 mM * 1 mL in DMSO		In-stock
5mg		In-stock
10mg		In-stock
25mg		In-stock

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生物活性

Ro 41-0960 is a CNS-penetrant, orally active catechol-O-methyl transferase (COMT) inhibitor. Ro 41-0960 reduces dopamine catabolism, increases striatal dopamine and DOPAC levels, decreases striatal HVA levels, induces apoptosis, inhibits proliferation and extracellular matrix formation in uterine fibroid cells. Ro 41-0960 arrests or shrinks uterine fibroid lesions in rats. Ro 41-0960 can be used for the research of Parkinson’s disease, uterine leiomyomas, and breast cancer[1].

体外研究

Ro 41-0960 (0.05-50 µM; 20 min) can directly activate SERCA2a in porcine myocardial sarcoplasmic reticulum microsomes, with an EC50 of 27 µM, and can also increase ATPase turnover rate by 38%.

Ro 41-0960 (0.5-100 µM; 30 min) exhibits a weak concentration dependent reverse effect on Ca2+transient amplitude and CaTD50 in cardiomyocytes derived from human induced pluripotent stem cells, with minimal impact on beat frequency.

Ro 41-0960 can inhibit catechol-O-methyltransferase (COMT) in rat brain with an IC50 of 16 nmol/L; Simultaneously, it can inhibit COMT in rat liver with an IC50 of 42 nmol/L.

Ro 41-0960 (30 min) can effectively inhibit COMT activity in the cytoplasmic components of healthy human breast tissue, with IC50 values ranging from 5.1 nM to 42.1 nM in 7 independent tissue samples, and its activity can be completely blocked at 0.3 μM.

Ro 41-0960 (10 μM; 5-6 h) can inhibit COMT activity in MCF-7 human breast tumor cells by about 98%, reduce the inactivation of catechol estrogen, and increase catechol estrogen induced DNA damage by about 200% without producing cytotoxicity.

体内研究

Ro 41-0960 (20 mg/kg; intraperitoneal injection; Single dose administration/daily administration; For 5 consecutive days, it is a COMT inhibitor that can penetrate the blood-brain barrier. In male Wistar rats, it can significantly increase the levels of striatal DA and DOPAC, and significantly reduce the level of striatal HVA [1].
Ro 41-0960 (150 mg/kg; subcutaneous injection; Twice a day; Lasting for 28 days, it can inhibit the growth or shrink of uterine fibroids in Eker rats [2].
Ro 41-0960 (30 mg/kg; intraperitoneal injection; Single dose administration can alleviate or completely prevent changes in the concentration of sulfur-containing amino acid metabolites in rat brain regions, peripheral tissues, and plasma induced by levodopa (L-Dopa) , while the effect on these metabolites is minimal when administered alone.

Animal Model:	Wistar rats (male, 270-320 g)
Dosage:	20 mg/kg
Administration:	i.p.; single dose (acute); daily; 5 days (chronic)
Result:	Produced a statistically significant 123.6% increase in striatal DA content, a 234.6% increase in striatal DOPAC content, and a 58.0% reduction in striatal HVA content relative to saline controls (acute treatment). Produced a 122.5% increase in striatal DA content, a 225.5% increase in striatal DOPAC content, and a 13.1% reduction in striatal HVA content relative to saline controls (chronic treatment). Caused a significantly greater reduction in HVA content compared to the acute treatment.

Animal Model:	Eker rats (female, 14-16 months old, germline mutation in tuberous sclerosis-2 tumor suppressor gene)
Dosage:	150 mg/kg
Administration:	s.c.; twice daily; 28 days
Result:	Exhibited fibroid volumes of 86% and 105% of initial burden at 2 and 4 weeks post-treatment, respectively. Increased the urinary 2-hydroxy E2/16-hydroxy E2 ratio. Increased p53 mRNA levels. Decreased PARP1-positive cells. Decreased PCNA-positive cells. Decreased cyclin D1-positive cells. Decreased TGFb3 mRNA levels. Did not alter normal tissue histology, serum liver enzyme levels (AST, ALT, total bilirubin), or urinary DPD levels.

Animal Model:	Sprague-Dawley rats (male, ~200 g)
Dosage:	30 mg/kg
Administration:	i.p.; single dose
Result:	Showed no significant difference in mean SAM and SAH concentrations in cortex, hippocampus, cerebellum, spleen, kidney, and liver. Increased mean striatal SAM concentration. Decreased mean striatal SAH concentration. Showed no significant difference in mean total plasma homocysteine concentration. Increased mean SAM concentrations significantly in cortex, hippocampus, cerebellum, striatum, spleen, and kidney.

分子式

C₁₃H₈FNO₅

分子量

277.2047632

CAS号

125628-97-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (360.75 mM)

* "≥" means soluble, but saturation unknown

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.6075 mL	18.0375 mL	36.0750 mL
5 mM	0.7215 mL	3.6075 mL	7.2150 mL
10 mM	0.3608 mL	1.8038 mL	3.6075 mL

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, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

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

1.

请依序添加每种溶剂： 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline

Solubility: ≥ 2.5 mg/mL (9.02 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (9.02 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。
2.

请依序添加每种溶剂： 10% DMSO → 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (9.02 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (9.02 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。

纯度： ≥98%

Data Sheet

SDS

产品使用指南

[1]. Elena Gallardo, et al. The effect of hydroxytyrosol and its nitroderivatives on catechol-O-methyl transferase activity in rat striatal tissue. RSC Adv., 2014, 4, 61086.

[2]. Hassan MH, et al. Towards non-surgical therapy for uterine fibroids: catechol-O-methyl transferase inhibitor shrinks uterine fibroid lesions in the Eker rat model. Hum Reprod. 2011;26(11):3008-3018.

The molarity calculator equation

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

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

Other Forms of Rapamycin:

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器