Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ropinirole hydrochloride (SKF-101468A) 是D3/D2受体激动剂,对 D2受体的Ki=29 nM。它对 hD2,hD3和 hD4受体的pEC50分别为 7.4、8.4 和 6.8。它对 D1受体没有亲和力。它对帕金森氏病具有潜在的研究价值。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
10 mg | ¥ 198 | 现货 | ||
25 mg | ¥ 327 | 现货 | ||
50 mg | ¥ 547 | 现货 | ||
100 mg | ¥ 970 | 现货 | ||
200 mg | ¥ 1,620 | 现货 | ||
500 mg | ¥ 2,730 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 271 | 现货 |
产品描述 | Ropinirole hydrochloride (SKF-101468A) is a selective dopamine D2 receptors agonist (Ki: 29 nM). Ropinirole hydrochloride (SKF-101468A) is the hydrochloride salt form of ropinirole, a non-ergot dopamine agonist with antiparkinsonian property. |
靶点活性 | D2 receptor:29 nM(Ki) |
体外活性 | Ropinirole scavenges free radicals and suppresses lipid peroxidation in the Fe2+–Water2 reaction system. [2] |
体内活性 | Ropinirole (50 mg/kg, i.p.) causes biphasic spontaneous locomotor activity in mice. Ropinirole (0.05-1.0 mg/kg SC) dose-dependently inhibits the dyskinesias induced by 2-di-n-propylamino-5,6-di-hydroxytetralin in mice. Ropirtirole, at doses of 1 and 10 μg, injected unilaterally directly into the striatum of the rat causes marked, contralateral (away from the side of injection) asymmetry and circling in mice. Ropinirole (0.05-1.0 mg/kg SC or 0.1 mg/kg PO) reverses all motor and behavioural deficits induced by MPTP in marmosets. [1] Ropinirole (2 mg/kg, i.p.) for 7 days increases GSH, catalase and SOD activities in the striatum and protected striatal dopaminergic neurons against 6-hydroxydopamine (6-OHDA) in mice. [2] Ropinirole (0.2 mg/kg, i.p.) improves the use of previously akinetic forelimb and produced robust circling behavior in lesioned rats with striatal over-expression of both D2R and D3R compared to lesioned animals that received blank vector. The subtherapeutic dose of ropinirole generates only modest motor effects in lesioned rats with sole over-expression of D2R or D3R. [3] Ropinirole (1-8 mg t.i.d.) is rapidly and completely absorbed with oral bioavailability of 55%, clearance of 780 mL/min, elimination half-life of 6 hours in healthy volunteer. Since the major route of elimination for Ropinirole is by the CYP enzyme system, mainly by CYP1A2 and also by CYP3A4, inhibition of the former and possibly the latter may reduce the agent's clearance and lead to drug accumulation. [4] Ropinirole (0.25 mg-4.0 mg per day) treatment significantly improves patients' ability to initiate sleep, the amount of stage 2 sleep and sleep adequacy compared with placebo. Periodic limb movements with arousal per hour decreases from 7.0 to 2.5 with ropinirole but increases from 4.2 to 6.0 with placebo. Periodic limb movements while awake per hour decreases from 56.5 to 23.6 with ropinirole but increases from 46.6 to 56.1 with placebo. [5] |
激酶实验 | PARP1 enzyme activity is measured by using a commercial assay kit with the exception that cell lysates containing wild-type PARP1 or PARP Y907 mutant are used in place of the PARP1 protein included with the kit. Total lysate (500 ng) is added to each reaction. The dose course of PARP inhibitor Veliparib (ABT-888) is from 0.01 to 1,000 μM. PARP enzyme activity of wild-type and mutants is determined after incubation with the substrate is measured using a plate reader[2]. |
别名 | SKF 101468 hydrochloride, SKF-101468A, Ropinirole HCl, 盐酸罗匹尼罗 |
分子量 | 296.84 |
分子式 | C16H24N2O·HCl |
CAS No. | 91374-20-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 14.8 mg/mL (50 mM)
H2O: 29.7 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / H2O | 1 mM | 3.3688 mL | 16.8441 mL | 33.6882 mL | 84.2205 mL |
5 mM | 0.6738 mL | 3.3688 mL | 6.7376 mL | 16.8441 mL | |
10 mM | 0.3369 mL | 1.6844 mL | 3.3688 mL | 8.422 mL | |
20 mM | 0.1684 mL | 0.8422 mL | 1.6844 mL | 4.211 mL | |
50 mM | 0.0674 mL | 0.3369 mL | 0.6738 mL | 1.6844 mL | |
H2O | 100 mM | 0.0337 mL | 0.1684 mL | 0.3369 mL | 0.8422 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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