1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. Calcium Channel nAChR
  3. ZSET1446

ZSET1446  (Synonyms: ST-101)

目录号: HY-11013 纯度: 98.01%
COA 产品使用指南

ZSET1446 是一种新颖的促进认知药,在不同的阿尔茨海默病模型中,能够改善学习功能障碍。

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ZSET1446 Chemical Structure

ZSET1446 Chemical Structure

CAS No. : 887603-94-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2599
In-stock
1 mg ¥900
In-stock
5 mg ¥2250
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10 mg ¥3150
In-stock
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100 mg   询价  

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Customer Review

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

ZSET1446 is a novel cognitive enhancer that significantly improves learning deficits in various types of Alzheimer disease (AD) models.

体外研究
(In Vitro)

ZSET1446 (100 pM-10 nM) exerts limited effects on the basal neuronal excitability and synaptic transmission. ZSET1446 potentiates the facilitatory effect of nAChR stimulation on sPSC frequency. ZSET1446 potentiates the increase in sIPSC frequency by local application of nicotine (5 µM; 2 minutes) without affecting the basal sIPSC frequency at the range of 10 pM to 1 nM[1].

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

体内研究
(In Vivo)

ZSET1446 enhances object recognition memory in mice and ameliorates cognitive impairment caused by scopolamine in rats. Concomitant administration of subeffective doses of ZSET1446 and memantine significantly ameliorates the cognitive performance in the novel object recognition task in both mice and rats. Moreover, oral administration of ZSET1446 or memantine increases the extracellular level of ACh in the hippocampus as compared with the control. Further, concomitant administration of subeffective doses of ZSET1446 and memantine significantly increases the extracellular level of ACh as compared with the group of ZSET1446 or memantine alone[2]. ZSET1446 (0.002, 0.01, and 0.1 mg/kg, p.o.) ameliorates cognitive deficits of SAMP8 after 4, 8, 12, and 16 weeks of treatment in a novel object recognition test. ZSET1446 also reduces grading scores of SAMP8 after 16 weeks of treatment. Further, 8-week treatment of ZSET1446 significantly reduces the total number of Aβ-positive granules in the hippocampus[3].

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

Clinical Trial
分子量

236.27

Formula

C15H12N2O

CAS 号
性状

固体

颜色

Light yellow to khaki

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (211.62 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.2324 mL 21.1622 mL 42.3245 mL
5 mM 0.8465 mL 4.2324 mL 8.4649 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 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 (10.58 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。

    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 (10.58 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。

    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。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):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

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)。
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
[2]

The experimental apparatus consists of a Plexiglas open-field box [25 cm (width) × 41 cm (length) × 17 cm (depth), model TP-105], the floor of which is covered with sawdust. The apparatus is located in a sound-attenuated room. The procedure for the novel object recognition task consists of three different sessions: habituation, training, and retention sessions. Each mouse is individually habituated to the box, with 10 min of exploration in the absence of objects (day 1: habituation session). ZSET1446 at doses of 0.001, 0.003, 0.01, and 0.03 mg/kg and/or memantine at doses of 3 and 10 mg/kg is orally administered 60 min before the training trial. In the experiment of injection of nicotinic receptor antagonists, oral administration of ZSET1446 and i.p. injection of mechamylamine or DHbE at each dose of 1 mg/kg are given 60 min before the training trial. During the training session, two different novel objects are symmetrically fixed to the floor in the box, and each animal is allowed to explore in the box for 10 min (day 2: training session). These objects are different in shape and color but similar in size. The mice are considered to be exploring the object when the mouse is facing, touching, or sniffing the object. The time spent for exploring each object is manuallymeasured by a stopwatch. In the training session, locomotor activity is simultaneously measured for a period of 10 min automatically, using an Animex Auto placed under the open-field box. After the training trial, mice are immediately returned to their home cages.

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

参考文献

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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.2324 mL 21.1622 mL 42.3245 mL 105.8111 mL
5 mM 0.8465 mL 4.2324 mL 8.4649 mL 21.1622 mL
10 mM 0.4232 mL 2.1162 mL 4.2324 mL 10.5811 mL
15 mM 0.2822 mL 1.4108 mL 2.8216 mL 7.0541 mL
20 mM 0.2116 mL 1.0581 mL 2.1162 mL 5.2906 mL
25 mM 0.1693 mL 0.8465 mL 1.6930 mL 4.2324 mL
30 mM 0.1411 mL 0.7054 mL 1.4108 mL 3.5270 mL
40 mM 0.1058 mL 0.5291 mL 1.0581 mL 2.6453 mL
50 mM 0.0846 mL 0.4232 mL 0.8465 mL 2.1162 mL
60 mM 0.0705 mL 0.3527 mL 0.7054 mL 1.7635 mL
80 mM 0.0529 mL 0.2645 mL 0.5291 mL 1.3226 mL
100 mM 0.0423 mL 0.2116 mL 0.4232 mL 1.0581 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.

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产品名称:
ZSET1446
目录号:
HY-11013
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