1. Neuronal Signaling
  2. Monoamine Oxidase
  3. 2614W94

2614W94是具有选择性的,可逆的monoamine oxidase-A抑制剂,IC50值和Ki值分别为5 nM和1.6 nM。

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2614W94 Chemical Structure

2614W94 Chemical Structure

CAS No. : 205187-35-5

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2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
1 mg ¥2340
In-stock
5 mg ¥4680
In-stock
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50 mg   询价  
100 mg   询价  

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Customer Review

查看 Monoamine Oxidase 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

2614W94 is a selective, reversible inhibitor of monoamine oxidase-A with a competitive mechanism of inhibition and IC50 of 5 nM and Ki of 1.6 nM with serotonin as substrate.

IC50 & Target

IC50: 5 nM (Monoamine Oxidase)[1]
Ki: 1.6 nM (Monoamine Oxidase)[1]

体外研究
(In Vitro)

2614W94 shows potent inhibitory activity against MAO-A, but shows no inhibition of MAO-B at 30 nM[1].

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

体内研究
(In Vivo)

2614W94 (5 mg/kg, p.o.) produces selective inhibition of MAO-A in brains and livers of rats. 2614W94 (5 mg/kg, p.o.) also causes an elevation of neurotransmitter amines in brain, inparticular serotonin and norepinephrine, with a concomitant decrease in their oxidized metabolites. 2614W94 (0.5, 1, 2 mg/kg, p.o.) potentiates 5-hydroxytryptophan-induced head twitches in rats in a dose-dependent manner, with an extrapolated ED50 of 1.1 mg/kg[1].

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

分子量

344.31

Formula

C15H11F3O4S

CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (290.44 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 2.9044 mL 14.5218 mL 29.0436 mL
5 mM 0.5809 mL 2.9044 mL 5.8087 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 (protect from light, stored under nitrogen)。-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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.26 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,此方案实验周期在半个月以上的动物实验酌情使用。

    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玉米油中,混合均匀。

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)。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

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
Kinase Assay
[1]

MAO-A and -B forms are assayed. Rat brain mito-chondrial extract is pre-incubated with the inhibitor for 15 min at 37°C in 50 mM potassium phosphate buffer (pH 7.4). Substrates [3H]serotonin (0.2 mM, 5 Ci/mol) and [14C]β-phene-thylamine (10 µM, 3 Ci/mol) are then added, and incubation at 37°C is continued for 20 min. Blank assays contain 2 mM pargyline to inhibit all MAO activity. The reaction is terminated with 0.2 mL of 2 N HCl, and products are extracted with 6 mL of ethyl acetate/toluene (1:1). A 4 mL aliquot of the organic layer is countedin 10 mL of Ecolite in a scintillation spectrometer programmed for double-label counting. Assays are performed in triplicate unless otherwise indicated. At the above concentrations, serotonin is a selective substrate for MAO-A, and β-phenethylamine is aselective substrate for MAO-B.

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

Animal Administration
[1]

Rats: Nonfasted Sprague-Dawley male rats (250-350 g) are dosed by gavage with 0.5% methyl cellulose or with 2614W94 or other compounds suspended in the methyl cellulose vehicle. For all groups, n = 3 unless otherwise specified. For oral administration, dosing volume is 10 mL/kg of body weight. For intravenous dosing, the vehicle is a mixture of PEG 400 (polyethylene glycol; molecular weight, 400), ethanol, and physiologic saline in a volume ratio of 1.5/1.5/1.0, respectively, and the dosing volume is 1 mL/kg. After dosing, rats are returned to their cages and allowed free access to water. Any animals kept overnight are also given food. Death is by CO2 asphyxiation, after which brains and livers are promptly removed, frozen on dry ice, and stored at -70°C.

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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-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 2.9044 mL 14.5218 mL 29.0436 mL 72.6090 mL
5 mM 0.5809 mL 2.9044 mL 5.8087 mL 14.5218 mL
10 mM 0.2904 mL 1.4522 mL 2.9044 mL 7.2609 mL
15 mM 0.1936 mL 0.9681 mL 1.9362 mL 4.8406 mL
20 mM 0.1452 mL 0.7261 mL 1.4522 mL 3.6304 mL
25 mM 0.1162 mL 0.5809 mL 1.1617 mL 2.9044 mL
30 mM 0.0968 mL 0.4841 mL 0.9681 mL 2.4203 mL
40 mM 0.0726 mL 0.3630 mL 0.7261 mL 1.8152 mL
50 mM 0.0581 mL 0.2904 mL 0.5809 mL 1.4522 mL
60 mM 0.0484 mL 0.2420 mL 0.4841 mL 1.2101 mL
80 mM 0.0363 mL 0.1815 mL 0.3630 mL 0.9076 mL
100 mM 0.0290 mL 0.1452 mL 0.2904 mL 0.7261 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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HY-101578
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