Idalopirdine
(Synonyms: Lu AE58054) 目录号 : GC36291A 5-HT6 receptor antagonist
Cas No.:467459-31-0
Sample solution is provided at 25 µL, 10mM.
LU AE58054 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 0.83 nM).1 It is selective for 5-HT6 over other 5-HT receptor subtypes (Kis = 250 to >10,000 nM) and 70 other targets but does bind to α1A- and α1B-adrenergic receptors (α1B-ARs; Kis = 21 and 22 nM, respectively). LU AE58054 (5-20 mg/kg) reverses phencyclidine-induced deficits in novel object recognition memory in rats. When administered in combination with the cholinesterase inhibitor rivastigmine , LU AE58054 has an additive effect on the decreased number of slips and falls made by rats with bilateral striatal-dopaminergic and cortical-cholinergic system lesions, a model of Parkinson’s disease motor disruption, in the Michigan complex motor control task.2
1.Arnt, J., Bang-Andersen, B., Grayson, B., et al.Lu AE58054, a 5-HT6 antagonist, reverses cognitive impairment induced by subchronic phencyclidine in a novel object recognition test in ratsInt. J. Neuropsychopharmacol.13(8)1021-1033(2010) 2.Cherian, A.K., Kucinski, A., Wu, R., et al.Co-treatment with rivastigmine and idalopirdine reduces the propensity for falls in a rat model of falls in Parkinson's diseasePsychopharmacology (Berl)236(6)1701-1715(2019)
Cas No. | 467459-31-0 | SDF | |
别名 | Lu AE58054 | ||
Canonical SMILES | FC1=CC(NC=C2CCNCC3=CC(OCC(F)(C(F)F)F)=CC=C3)=C2C=C1 | ||
分子式 | C20H19F5N2O | 分子量 | 398.37 |
溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml | 储存条件 | Store at -20°C |
General tips | 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.5102 mL | 12.5511 mL | 25.1023 mL |
5 mM | 0.502 mL | 2.5102 mL | 5.0205 mL |
10 mM | 0.251 mL | 1.2551 mL | 2.5102 mL |
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 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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,
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 saline,混匀澄清。
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。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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