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- 技术资料
- CAS号：
99755-59-6
- 规格：
1mLx10mM(inDMSO)/1mg/5mg/10mg/25mg/50mg/100mg/200mg/500mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥333.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥158.0 |
| 规格： | 5mg | 产品价格： | ￥330.0 |
| 规格： | 10mg | 产品价格： | ￥501.0 |
| 规格： | 25mg | 产品价格： | ￥1008.0 |
| 规格： | 50mg | 产品价格： | ￥1856.0 |
| 规格： | 100mg | 产品价格： | ￥2624.0 |
| 规格： | 200mg | 产品价格： | ￥3752.0 |
| 规格： | 500mg | 产品价格： | ￥5776.0 |
Product Introduction
Bioactivity
| 名称 | Rotigotine- |
| 描述 | Rotigotine (N-0923) is a non-ergot dopamine receptor agonist used in the therapy of Parkinson disease and restless leg syndrome. Administered as a once-daily transdermal patch, Rotigotine has not been associated with serum enzyme elevations during treatment or with episodes of clinically apparent liver injury. |
| 激酶实验 | 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. |
| 体外活性 | Rotigotine对D3 (pKi 9.2) 受体的选择性是D2/D4/D5 (pKi 8.5-8.0) 的10倍高，而对D1受体 (pKi 7.2) 则高出100倍。在原代中脑细胞培养中，Rotigotine (10 μM) 使THir神经元数量减少了40%。在功能性研究中，Rotigotine作为所有多巴胺受体的全效激动剂，但值得注意的是，其对D1受体的激活效力与对D2/D3受体相似 (pEC50 分别为：9.0, 9.4-8.6, 9.7)。Rotigotine (0.01 μM) 轻微保护多巴胺神经元免受MPP+毒性的影响，显著保护多巴胺神经元免受罗腾隆引起的细胞死亡，并显著抑制罗腾隆诱导的ROS产生。 |
| 体内活性 | 在经过预处理的大鼠中，Rotigotine（0.035/0.1/0.35 mg/kg）以剂量依赖的方式诱导对侧转向行为。相比之下，在未经药物处理的大鼠中，无论是单独使用Rotigotine还是与SCH 39166合用，所诱导的转向行为均较预处理的大鼠减少。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 250 mg/mL (792.47 mM), Sonication is recommended. Ethanol : 59 mg/mL (187.02 mM), Sonication is recommended. 10% DMSO+90% Saline : < 10 mg/mL (31.7 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (31.7 mM), Solution. |
| 关键字 | α2B-adrenergic | SPM-962 | SPM962 | Serotonin Receptor | Rotigotine- | Rotigotine | receptor | N0923 | N0437 | N 0923 | N 0437 | Inhibitor | inhibit | DopamineReceptor | Dopamine Receptor | dopamine | D3 | D2 | Beta Receptor | AdrenergicReceptor | Adrenergic Receptor | 5-hydroxytryptamine Receptor | 5HTReceptor | 5-HT1A | 5-HT Receptor | 5HT Receptor |
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罗替戈汀【99755-59-6】
￥158 - 5776
