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Encenicline hydrochloride

产品编号 T2285 CAS 550999-74-1

别名: (R)-7-氯-N-(奎宁环-3-基)苯并[b]噻吩-2-甲酰胺盐酸盐, EVP-6124 (hydrochloride), EVP-6124 hydrochloride

Encenicline hydrochloride (EVP-6124 hydrochloride) 是一种新型的α7神经元烟碱乙酰胆碱受体激动剂。

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Encenicline hydrochloride Chemical Structure

Encenicline hydrochloride, CAS 550999-74-1

规格	价格/CNY	货期
1 mg	￥ 1,080	现货
2 mg	￥ 1,470	现货
5 mg	￥ 2,190	现货
10 mg	￥ 2,850	现货
25 mg	￥ 4,730	现货
50 mg	￥ 6,760	现货
100 mg	￥ 9,170	现货
1 mL * 10 mM (in DMSO)	￥ 2,310	现货

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其他形式的 Encenicline hydrochloride:

Encenicline
现货

选择批次

纯度: 99.85%

纯度: 98.73%

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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 hydrochloride (EVP-6124 hydrochloride) is a new-type partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs).
体外活性	EVP-6124 hydrochloride displaces [3H]-MLA (Methyllycaconitine) (Ki=9.98 nM, pIC50=7.65±0.06, n=3) and [125I]-α-bungarotoxin (Ki=4.33 nM, pIC50=8.07±0.04, n=3). EVP-6124 is approximately 300 fold more potent than the natural agonist ACh (Ki=3 μM), measured in binding assays using [3H]-MLA. EVP-6124 inhibits the 5-HT3 receptor by 51% at 10 nM, the lowest concentration tested. Evaluation of the human 5-HT2B receptor expressed in CHO cells demonstrates displacement of [3H]-mesulergine (Ki=14 nM) and only antagonist activity in the rat gastric fundus assay at an IC50 of 16 μM. In binding and functional experiments, EVP-6124 shows selectivity for α7 nAChRs and does not activate or inhibit heteromeric α4β2 nAChRs[1].
体内活性	EVP-6124 hydrochloride has good brain penetration and an adequate exposure time. EVP-6124 (0.3 mg/kg, p.o.) significantly restores memory function in scopolamine-treated rats (0.1 mg/kg, i.p.) 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, p.o. This improvement is blocked by the selective α7 nAChR antagonist methyllycaconitine (0.3 mg/kg, i.p. or 10 μg, i.c.v.). EVP-6124 is found to bind moderately to rat plasma proteins with a mean fu of 0.11±0.01 (mean±SD) or 11%. Over a range of 0.1-30 mg/kg, p.o., EVP-6124 demonstrates proportional dose escalation. Tmax is at 4 h in plasma and 2 h brain, although the brain concentrations remained similar between 2 and 8 h. The B:P ratios are 1.7-5.1 between 1 and 8 h[1]. Pharmacokinetic studies have shown that EVP-6124 (0.4 mg/kg, i.p.) reaches peak brain concentration 2 hr after administration and remains at effective concentrations for at least 4 hr. EVP-6124 is administered to WT mice at ZT0 (0.4 mg/kg i.p single dose) and significantly increases the saturation index of NMDARs in slices obtained 4 hr later without causing prolonged wakefulness or enhanced locomotor activity [2].
激酶实验	Binding or activity of EVP-6124 is measured at 10 μM in a selectivity panel according to standard validated protocols under conditions defined by the contractor. For the 5-HT2A receptor binding assay, membranes are prepared from HEK293 cellsexpressing the human recombinant 5-HT2A receptor. For 5-HT2B and 5-HT2C receptor binding assays, membranes are prepared from CHO cells expressing the human recombinant 5-HT2B or 5-HT2C receptor. Affinity is determined by incubating different concentrations of EVP-6124 in binding buffer for 1 h. For 5-HT2A binding, the incubation is at 22°C in the presence of 0.5 nM [3H]-ketanserin; for 5-HT2B, at 22°C in the presence of 2 nM [3H]-mesulergine; and for 5-HT2C, at 37°C in the presence of 1 nM [3H]-mesulergine. Nonspecific binding is determined in the presence of 1 μM ketanserin, 10 μM mesulergine, or 10 μM RS-102221 for 5-HT2A, 5-HT2B, or 5-HT2C, respectively. All measurements are performed in triplicate. EVP-6124 is also tested in the 5-HT2B rat gastric fundus tissue response assay. Briefly, inhibition of α-methyl serotonin-induced contraction is isometrically measured. All measurements are performed in duplicate[1].

别名	(R)-7-氯-N-(奎宁环-3-基)苯并[b]噻吩-2-甲酰胺盐酸盐, EVP-6124 (hydrochloride), EVP-6124 hydrochloride
分子量	357.3
分子式	C16H17ClN2OS·HCl
CAS No.	550999-74-1

存储

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

溶解度

DMSO: 10 mg/mL (27.99 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	2.7988 mL	13.9938 mL	27.9877 mL	69.9692 mL
	5 mM	0.5598 mL	2.7988 mL	5.5975 mL	13.9938 mL
	10 mM	0.2799 mL	1.3994 mL	2.7988 mL	6.9969 mL
	20 mM	0.1399 mL	0.6997 mL	1.3994 mL	3.4985 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

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

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质量

配液浓度

参考文献

1. Prickaerts, J., van Goethem, N., Chesworth, R., Shapiro, G., Boess, F., & Methfessel, C. et al. (2012). 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. Neuropharmacology, 62(2), 1099-1110. doi: 10.1016/j.neuropharm.2011.10.024 2. Thomas Papouin, et al. Septal Cholinergic Neuromodulation Tunes the Astrocyte-Dependent Gating of Hippocampal NMDA Receptors to Wakefulness. Neuron. 2017 May 17;94:1-15.

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 hydrochloride 550999-74-1 Neuroscience AChR Encenicline Hydrochloride Nicotinic acetylcholine receptors EVP 6124 (R)-7-氯-N-(奎宁环-3-基)苯并[b]噻吩-2-甲酰胺盐酸盐 EVP-6124 (hydrochloride) EVP-6124 EVP6124 EVP-6124 hydrochloride Encenicline inhibit EVP-6124 Hydrochloride nAChR Inhibitor EVP 6124 Hydrochloride EVP6124 Hydrochloride inhibitor

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Encenicline hydrochloride

存储

溶解度

溶液配制表

计算器

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参考文献

相关产品

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剂量换算

体内实验配液计算器

技术支持

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