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Encenicline

产品编号 T7193 CAS 550999-75-2

别名: EVP-6124

Encenicline (EVP-6124) 是一种新型α7神经元烟碱乙酰胆碱受体 (nAChRs)激动剂，用于治疗精神分裂症和阿尔茨海默病的认知障碍。

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Encenicline, CAS 550999-75-2

规格	价格/CNY	货期
1 mg	￥ 897	现货
2 mg	￥ 1,280	现货
5 mg	￥ 2,190	现货
10 mg	￥ 2,830	现货
25 mg	￥ 4,690	现货
50 mg	￥ 6,720	现货
100 mg	￥ 9,120	现货
1 mL * 10 mM (in DMSO)	￥ 1,850	现货

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其他形式的 Encenicline:

Encenicline hydrochloride
现货

选择批次

纯度: 98%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Encenicline (EVP-6124) is a selective α7 nicotinic acetylcholine receptor (nAChRs) agonist in development for treating cognitive impairment in schizophrenia and Alzheimer's disease.
体外活性	In co-application experiments of EVP-6124 with acetylcholine, sustained exposure to EVP-6124 in functional investigations in oocytes caused desensitization at concentrations greater than 3 nM, while lower concentrations (0.3-1 nM) caused an increase in the acetylcholine-evoked response.?These actions were interpreted as representing a co-agonist activity of EVP-6124 with acetylcholine on α7 nAChRs.?The concentrations of EVP-6124 that resulted in physiological potentiation were consistent with the free drug concentrations in brain that improved memory performance in the ORT[2].
体内活性	EVP-6124 showed selectivity for α7 nAChRs and did not activate or inhibit heteromeric α4β2 nAChRs.?EVP-6124 had good brain penetration and an adequate exposure time.?EVP-6124 (0.3 mg/kg) significantly restored memory function in scopolamine-treated rats (0.1 mg/kg) in an object recognition task (ORT).?Although donepezil at 0.1 mg/kg, p.o. or EVP-6124 at 0.03 mg/kg, p.o. did not improve memory in this task, co-administration of these sub-efficacious doses fully restored memory.?In a natural forgetting test, an ORT with a 24 h retention time, EVP-6124 improved memory at 0.3 mg/kg, This improvement was blocked by the selective α7 nAChR antagonist methyllycaconitine (0.3 mg/kg or 10 μg)[1].
细胞实验	Experiments were carried out with human a7 nAChRs expressed in Xenopus laevis oocytes.?Oocytes were prepared, injected with cDNA encoding a7 nAChR subunits, and recorded using standard procedures.?Additional studies were carried out with rat a3b4, a4b2, and muscle a1b1gd nAChRs expressed in oocytes.?Briefly, ovaries were harvested from X. laevis females that were deeply anesthetized by cooling at 4℃ and with tricaine mesylate (3-aminobenzoic acid ethyl ester, methane sulfonate salt, 150 mg/l).?Small pieces of ovary were isolated in sterile Barth solution (88 mM NaCl, 1 mM KCl, 2.4 mM NaHCO3, 10 mM HEPES, 0.82 mM MgSO4·7H2O, 0.33 mM Ca(NO3)2·4H2O, and 0.41 mM CaCl2·6H2O, pH 7.4) and supplemented with 20 mg/ml kanamycin, 100 μg/ml penicillin, and 100 mg/ml streptomycin.?Injections of cDNAs encoding for the receptors were performed in at least one hundred oocytes using an automated ?injection device;?and receptor expression was examined at least two days later.?Oocytes were impaled with two electrodes filled with 3 M KCl, and their membrane potentials were ?maintained at ?80 mV throughout the experiment.?All recordings were performed ?at 18 C and cells were superfused with OR2 medium (82.5 mM NaCl, 2.5 mM KCl, 5 mM HEPES, 1.8 mM CaCl2·2H2O, and 1 mM MgCl2·6H2O, pH 7.4).?Currents were recorded using an automated process equipped with standard two-electrode voltage-clamp configuration.Data were captured and analyzed using Matlab or Excel software.ACh and EVP-6124 were prepared as concentrated stock solutions in water and then diluted in the recording medium to obtain the desired test concentrations.?All experiments were carried out using three or more cells[1].
动物实验	For the experiments using natural forgetting (a 24 h retention interval) and MLA, twenty-four 2-month-old male Wistar rats .?In the doseeresponse experiment, the rats were 2.5 months old (average body weight: 319 g). For the coadministration of EVP-6124 and MLA , the rats were 3 months old (average body weight: 357 g). For the co-administration of EVP-6124 and MLA, the rats were 4 months old (average body weight: 407 g). Across the 3 experiments, rats were tested a total of 5e10 times.?The effects of EVP-6124 on memory consolidation in particular were investigated in the natural forgetting test in the ORT, using twentyfour 3-month-old Wistar rats (average body weight: 357 g). All 24 rats received each treatment, i.e. each rat was tested 7 times in two experiments.?All animals were housed individually, which improves ORT performance, in standard type III Makrolon cages on sawdust bedding.?The animals were on a reversed 12/12-h light/dark cycle (lights on from 19:00 to 7:00 h);?and food and water were given ad libitum.?The rats were housed and tested in the same room.?A radio, playing softly provided background noise to mask noises in the room.?All testing was performed between 9:00 and 18:00 h under low illumination (20 lux)[1].

别名	EVP-6124
分子量	320.84
分子式	C16H17ClN2OS
CAS No.	550999-75-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 60 mg/mL (187.01 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.1168 mL	15.5841 mL	31.1682 mL	77.9205 mL
	5 mM	0.6234 mL	3.1168 mL	6.2336 mL	15.5841 mL
	10 mM	0.3117 mL	1.5584 mL	3.1168 mL	7.792 mL
	20 mM	0.1558 mL	0.7792 mL	1.5584 mL	3.896 mL
	50 mM	0.0623 mL	0.3117 mL	0.6234 mL	1.5584 mL
	100 mM	0.0312 mL	0.1558 mL	0.3117 mL	0.7792 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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参考文献

1. Prickaerts J, van Goethem NP, Chesworth R,et al.EVP-6124, a novel and selective α7 nicotinic acetylcholine receptor partial agonist, improves memory performance by potentiating the acetylcholine response of α7 nicotinic acetylcholine receptors[J].Neuropharmacology. 2012 Feb;62(2):1099-110. 2. Hayward A , Adamson L , Neill J C . Partial agonism at the α7 nicotinic acetylcholine receptor improves attention, impulsive action and vigilance in low attentive rats[J]. European Neuropsychopharmacology, 2017, 27(4):325-335.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

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。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

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。

Keywords

Encenicline 550999-75-2 Neuroscience AChR inhibit nAChR Nicotinic acetylcholine receptors EVP 6124 EVP6124 EVP-6124 Inhibitor inhibitor

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Encenicline

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

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