Rotigotine Hydrochloride (Synonyms: 罗替戈汀盐酸盐; N-0923 Hydrochloride)

目录号: HY-A0007 纯度: 99.65%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Rotigotine Hydrochloride (N-0923 Hydrochloride) 是 dopamine receptor 纯激动剂，是 5-HT1A receptor 的部分激动剂，以及 α2B-adrenergic receptor 的拮抗剂，K_i 值分别为 0.71 nM (dopamine D3 receptor)，4-15 nM (D2，D5，D4 receptors)，83 nM (dopamine D1 receptor)。

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Rotigotine Hydrochloride Chemical Structure

CAS No. : 125572-93-2

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥389	In-stock
5 mg	￥354	In-stock
10 mg	￥504	In-stock
25 mg	￥857	In-stock
50 mg	￥1200	In-stock
100 mg	￥1680	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Other Forms of Rotigotine Hydrochloride:

MCE 顾客使用本产品发表的 1 篇科研文献

•Clin Chem. 2019 Dec;65(12):1522-1531. [Abstract]

Rotigotine Hydrochloride 相关产品

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查看 Dopamine Receptor 亚型特异性产品:

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Dopamine Receptor D₁ Receptor D₂ Receptor D₃ Receptor D₄ Receptor D₅ Receptor

查看 Adrenergic Receptor 亚型特异性产品:

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α adrenergic receptor β adrenergic receptor

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5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor 5-HT Receptor

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Rotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with K_i of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

IC₅₀ & Target

D₃ Receptor

0.71 nM (Ki)

D₂ Receptor

4-15 nM (Ki)

D₅ Receptor

4-15 nM (Ki)

D₄ Receptor

4-15 nM (Ki)

D₁ Receptor

83 nM (Ki)

α1A

176 nM (Ki)

α1B

273 nM (Ki)

α2A

338 nM (Ki)

α2B

27 nM (Ki)

5-HT_1A Receptor

30 nM (Ki)

5-HT₇ Receptor

86 nM (Ki)

体外研究
(In Vitro)

Rotigotine (N-0923) has a 10-fold selectivity for D3 (pK_i 9.2) receptors compared with D2, D4 and D5 (pK_i 8.5-8.0) and a 100-fold selectivity compared with D1 receptors (pK_i 7.2). In functional studies, Rotigotine (N-0923) behaves as full agonist at all dopamine receptors but notably the potency for stimulation of D1 receptors is similar to that for D2 and D3 receptors (pEC₅₀ respectively: 9.0, 9.4-8.6, 9.7)^[1]. Rotigotine (N-0923) (10 µM) decreases the number of THir neurons by 40% in primary mesencephalic cell culture. Rotigotine (0.01 µM) slightly protects dopaminergic neurons against MPP⁺ toxicity, significantly protects dopaminergic neurons against rotenone-induced cell death, and significantly inhibits ROS production by rotenone^[4].

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

体内研究
(In Vivo)

In primed rats, Rotigotine (N-0923) (0.035, 0.1 and 0.35 mg/kg) induces contralateral turning behavior in a dose dependent manner. In drug naive rats, the turning behavior induced by Rotigotine, either alone or in combination with SCH 39166, is reduced compared to primed rats^[3].

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

Clinical Trial

分子量

351.93

Formula

C₁₉H₂₆ClNOS

CAS 号

125572-93-2

性状

固体

颜色

White to off-white

中文名称

罗替戈汀盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 50 mg/mL (142.07 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : 4.76 mg/mL (13.53 mM; 超声助溶 (<60°C))

* "≥" 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	2.8415 mL	14.2074 mL	28.4147 mL
5 mM	0.5683 mL	2.8415 mL	5.6829 mL
10 mM	0.2841 mL	1.4207 mL	2.8415 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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 (7.10 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 (7.10 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。
20% SBE-β-CD in Saline 的配制（4°C，储存一周）：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。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.10 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，此方案实验周期在半个月以上的动物实验酌情使用。
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玉米油中，混合均匀。

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）。

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 99.65%

选择批次：

Data Sheet (629 KB) SDS (393 KB)

COA (287 KB) RP-HPLC (242 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Wood M, et al. Rotigotine is a potent agonist at dopamine D1 receptors as well as at dopamine D2 and D3 receptors. Br J Pharmacol. 2015 Feb;172(4):1124-35. [Content Brief]

[2]. Scheller D, et al. The in vitro receptor profile of rotigotine: a new agent for the treatment of Parkinson's disease. Naunyn Schmiedebergs Arch Pharmacol. 2009 Jan;379(1):73-86. [Content Brief]

[3]. Fenu S, et al. In vivo dopamine agonist properties of rotigotine: Role of D1 and D2 receptors. Eur J Pharmacol. 2016 Oct 5;788:183-91. [Content Brief]

[4]. Radad K, et al. Neuroprotective effect of rotigotine against complex I inhibitors, MPP? and rotenone, in primary mesencephalic cell culture. Folia Neuropathol. 2014;52(2):179-86. [Content Brief]

Kinase Assay ^[1]	Binding assays are performed in 96-well polypropylene tubes in a final volume of 2 mL for D1 and D4 membranes and 1 mL for D2, D3 and D5 membranes containing: 50 μL radioligand, 10 μL drug/buffer/non-specific binding, buffer (final concentration 50 mM Tris-HCl pH 7.4, MgCl₂ 2 mM) and membranes (5 μg protein for D2 and D3 and 25 μg protein for D1 and D5). Following 120 min of incubation at 25°C, bound radioligand is determined by rapid vacuum filtration through A/C glass fibre filters presoaked in 0.1% polyethylenimine. The filters are washed four times with 2 mL ice-cold ishing buffer (Tris-HCl 50 mM, pH 7.4 at 4°C) and retained radioactivity is determined by liquid scintillation counting. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Primed rats: Two weeks after the 6-OHDA lesions, rats are primed with apomorphine (0.5 mg/kg s.c.). Rats showing less than 150 contralateral rotations during the 1 h testing period are excluded from the study. Three days after priming, rats are divided into different experimental groups and treated with different doses of the dopamine receptor agonists (Rotigotine or pramipexole) alone or in combination with dopamine D₁ (SCH 39166) or D₂ (eticlopride) receptor antagonists as reported: saline+Rotigotine (0.035 mg/kg s.c., n=9; 0.1 mg/kg s.c., n=9; 0.35 mg/kg s.c., n=8); SCH 39166 (0.1 mg/kg s.c.)+Rotigotine (0.035 mg/kg s.c., n=5; 0.1 mg/kg s.c., n=7; 0.35 mg/kg s.c., n=5); eticlopride (0.1 mg/kg s.c.) + Rotigotine (0.1 mg/kg s.c., n=5; 0.35 mg/kg s.c., n=5); Saline+pramipexole (0.035 mg/kg s.c., n=5; 0.1 mg/kg s.c., n=12; 0.35 mg/kg s.c., n=7); SCH 39166 (0.1 mg/kg s.c.)+pramipexole (0.035 mg/kg s.c., n=5; 0.1 mg/kg s.c., n=6; 0.35 mg/kg s.c., n=6); eticlopride (0.1 mg/kg s.c.)+pramipexole (0.1 mg/kg s.c., n=7; 0.35 mg/kg s.c., n=5). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Wood M, et al. Rotigotine is a potent agonist at dopamine D1 receptors as well as at dopamine D2 and D3 receptors. Br J Pharmacol. 2015 Feb;172(4):1124-35. [Content Brief] [2]. Scheller D, et al. The in vitro receptor profile of rotigotine: a new agent for the treatment of Parkinson's disease. Naunyn Schmiedebergs Arch Pharmacol. 2009 Jan;379(1):73-86. [Content Brief] [3]. Fenu S, et al. In vivo dopamine agonist properties of rotigotine: Role of D1 and D2 receptors. Eur J Pharmacol. 2016 Oct 5;788:183-91. [Content Brief] [4]. Radad K, et al. Neuroprotective effect of rotigotine against complex I inhibitors, MPP? and rotenone, in primary mesencephalic cell culture. Folia Neuropathol. 2014;52(2):179-86. [Content Brief]

Rotigotine Hydrochloride 相关分类

Neurological Disease

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

H₂O / DMSO	1 mM	2.8415 mL	14.2074 mL	28.4147 mL	71.0369 mL
	5 mM	0.5683 mL	2.8415 mL	5.6829 mL	14.2074 mL
	10 mM	0.2841 mL	1.4207 mL	2.8415 mL	7.1037 mL
DMSO	15 mM	0.1894 mL	0.9472 mL	1.8943 mL	4.7358 mL
	20 mM	0.1421 mL	0.7104 mL	1.4207 mL	3.5518 mL
	25 mM	0.1137 mL	0.5683 mL	1.1366 mL	2.8415 mL
	30 mM	0.0947 mL	0.4736 mL	0.9472 mL	2.3679 mL
	40 mM	0.0710 mL	0.3552 mL	0.7104 mL	1.7759 mL
	50 mM	0.0568 mL	0.2841 mL	0.5683 mL	1.4207 mL
	60 mM	0.0474 mL	0.2368 mL	0.4736 mL	1.1839 mL
	80 mM	0.0355 mL	0.1776 mL	0.3552 mL	0.8880 mL
	100 mM	0.0284 mL	0.1421 mL	0.2841 mL	0.7104 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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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.

Keywords:

Rotigotine125572-93-2N-0923罗替戈汀盐酸盐N0923N 0923Dopamine ReceptorAdrenergic Receptor5-HT ReceptorBeta ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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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)

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Rotigotine Hydrochloride (Synonyms: 罗替戈汀盐酸盐; N-0923 Hydrochloride)

Other Forms of Rotigotine Hydrochloride:

MCE 顾客使用本产品发表的 1 篇科研文献