2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. nAChR
  4. Encenicline hydrochloride

Encenicline hydrochloride  (Synonyms: EVP-6124 hydrochloride)

目录号: HY-15430A 纯度: 98.77%
COA 产品使用指南

摩尔计算器

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

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Encenicline hydrochloride Chemical Structure

Encenicline hydrochloride Chemical Structure

CAS No. : 550999-74-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2530
In-stock
5 mg ￥2300
In-stock
10 mg ￥3335
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50 mg 现货 询价
100 mg   询价  
200 mg   询价  

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Customer Review

Other Forms of Encenicline hydrochloride:

Encenicline hydrochloride 相关抗体

Top Publications Citing Use of Products

    Encenicline hydrochloride purchased from MCE. Usage Cited in: Eur J Pharmacol. 2017 Sep 15;811:110-116.  [Abstract]

    Effects of EVP-6124 on the novel object recognition test in rats. EVP-6124 (0.3-1 mg/kg) is orally administered 1 h before the acquisition trial.

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Encenicline hydrochloride (EVP-6124 hydrochloride) is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs).

    IC50 & Target

    α7 nAChR[1]
    体外研究
    (In Vitro)

    Encenicline (EVP-6124) 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). Encenicline (EVP-6124) is approximately 300 fold more potent than the natural agonist ACh (Ki=3 μM), measured in binding assays using [3H]-MLA. Encenicline hydrochloride 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, Encenicline (EVP-6124) shows selectivity for α7 nAChRs and does not activate or inhibit heteromeric α4β2 nAChRs[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Encenicline hydrochloride 相关抗体:
    体内研究
    (In Vivo)

    Encenicline hydrochloride has good brain penetration and an adequate exposure time. Encenicline hydrochloride (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 Encenicline hydrochloride 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, Encenicline hydrochloride 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.). Encenicline hydrochloride 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., Encenicline hydrochloride 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 Encenicline hydrochloride (0.4 mg/kg, i.p.) reaches peak brain concentration 2 hr after administration and remains at effective concentrations for at least 4 hr. Encenicline hydrochloride 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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    分子量

    357.30

    Formula

    C16H18Cl2N2OS
    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : ≥ 50 mg/mL (139.94 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.7988 mL 13.9938 mL 27.9877 mL
    5 mM 0.5598 mL 2.7988 mL 5.5975 mL
    查看完整储备液配制表

    * 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (7.00 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (7.00 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料
    参考文献
    Animal Administration
    [1][2]

    Rats[1]
    Twenty-four 2.5-month-old male Wistar rats (average body weight: 329 g) are used. Before testing EVP-6124, the effects of scopolamine alone at 0.03, 0.1, or 0.3 mg/kg, i.p. in the ORT are determined (n=8 per treatment). Scopolamine (0.1 mg/kg, i.p.) injected 30 min before T1 resulted in a robust deficit at T2 when a 1 h interval is used. The d2 index is not significantly different from the chance level of performance; and there are no changes in exploratory behavior for 0.1 mg/kg, i.p. of scopolamine compared with saline. Subsequently, the ability of Encenicline (EVP-6124) to reverse the memory impairment induced by 0.1 mg/kg of scopolamine is tested. First, scopolamine and then Encenicline (EVP-6124) (0.03, 0.1, 0.3, and 1.0 mg/kg, p.o.) are administered 30 min before T1. For the control treatments, animals received either deionized water (p.o.) plus saline (i.p.) or deionized water (p.o.) plus 0.1 mg/kg scopolamine (i.p.).
    Mice[2]
    Adult male mice (3-6 months old) are used throughout this study. Encenicline (EVP-6124) is injected i.p. (0.4 mg/kg) at Zeitgeber time (ZT0) in awake mice (9 mice total for this experiment), in the animal facility. Mice are then immediately returned to their home cage with their siblings and left undisturbed for 4 hr (ZT4). During this time, they are closely monitored to check for possible behavioral effects of Encenicline (EVP-6124) injection. All of the 9 injected mice nested and are immobile in the hour following the injection.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    Encenicline hydrochloride 相关分类

    完整储备液配制表

    * 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

    可选溶剂 浓度 溶剂体积 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
    15 mM 0.1866 mL 0.9329 mL 1.8658 mL 4.6646 mL
    20 mM 0.1399 mL 0.6997 mL 1.3994 mL 3.4985 mL
    25 mM 0.1120 mL 0.5598 mL 1.1195 mL 2.7988 mL
    30 mM 0.0933 mL 0.4665 mL 0.9329 mL 2.3323 mL
    40 mM 0.0700 mL 0.3498 mL 0.6997 mL 1.7492 mL
    50 mM 0.0560 mL 0.2799 mL 0.5598 mL 1.3994 mL
    60 mM 0.0466 mL 0.2332 mL 0.4665 mL 1.1662 mL
    80 mM 0.0350 mL 0.1749 mL 0.3498 mL 0.8746 mL
    100 mM 0.0280 mL 0.1399 mL 0.2799 mL 0.6997 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Encenicline550999-74-1EVP-6124EVP6124EVP 6124nAChRNicotinic acetylcholine receptorsInhibitorinhibitorinhibit

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