2. Membrane Transporter/Ion Channel
  3. Monoamine Transporter Sodium Channel
  4. Nisoxetine

Nisoxetine  (Synonyms: 尼索西汀)

目录号: HY-B1704 纯度: 98.28%
COA 产品使用指南

摩尔计算器

Nisoxetine 是一种有效的和选择性的去甲肾上腺素转运蛋白 (NET) 抑制剂，Kd 值为 0.76 nM。Nisoxetine 是一种抗抑郁试剂和局部麻药，它可以阻断电压门控性钠通道。

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Nisoxetine Chemical Structure

Nisoxetine Chemical Structure

CAS No. : 53179-07-0

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Other Forms of Nisoxetine:

Nisoxetine 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Nisoxetine is a potent and selective inhibitor of noradrenaline transporter (NET), with a Kd of 0.76 nM. Nisoxetine is an antidepressant and local anesthetic, it can block voltage-gated sodium channels[1][2][3].

IC50 & Target

Kd: 0.76 nM (NET)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
1150 nM
Compound: nisoxetine
Inhibition of human DAT expressed in HEK293 cells assessed as inhibition of dopamine reuptake after 30 mins by fluorescence assay
Inhibition of human DAT expressed in HEK293 cells assessed as inhibition of dopamine reuptake after 30 mins by fluorescence assay
[PMID: 22938049]
HEK293 IC50
1150 nM
Compound: Nisoxetine
Inhibition of human DAT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay
Inhibition of human DAT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay
[PMID: 25221656]
HEK293 IC50
1150 nM
Compound: Nisoxetine
Inhibition of DA reuptake at human DAT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
Inhibition of DA reuptake at human DAT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
[PMID: 24974340]
HEK293 IC50
18 nM
Compound: nisoxetine
Inhibition of human NET expressed in HEK293 cells assessed as inhibition of noradrenaline reuptake after 30 mins by fluorescence assay
Inhibition of human NET expressed in HEK293 cells assessed as inhibition of noradrenaline reuptake after 30 mins by fluorescence assay
[PMID: 22938049]
HEK293 IC50
20 nM
Compound: Nisoxetine
Inhibition of human NET expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay
Inhibition of human NET expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay
[PMID: 25221656]
HEK293 IC50
20 nM
Compound: Nisoxetine
Inhibition of norepinephrine reuptake at human NET expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
Inhibition of norepinephrine reuptake at human NET expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
[PMID: 24974340]
HEK293 IC50
700 nM
Compound: nisoxetine
Inhibition of human SERT expressed in HEK293 cells assessed as inhibition of serotonin reuptake after 30 mins by fluorescence assay
Inhibition of human SERT expressed in HEK293 cells assessed as inhibition of serotonin reuptake after 30 mins by fluorescence assay
[PMID: 22938049]
HEK293 IC50
700 nM
Compound: Nisoxetine
Inhibition of human SERT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay
Inhibition of human SERT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay
[PMID: 25221656]
HEK293 IC50
700 nM
Compound: Nisoxetine
Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
[PMID: 24974340]
MDCK IC50
8.3 nM
Compound: Nisoxetine
Inhibition of [3H]norepinephrine reuptake at human NET expressed in MDCK cells by scintillation counting
Inhibition of [3H]norepinephrine reuptake at human NET expressed in MDCK cells by scintillation counting
[PMID: 21093273]
体外研究
(In Vitro)

Nisoxetine 抑制 [3H]Nisoxetine 与大鼠额叶皮层膜的结合，Ki 为 1.4±0.1 nM[2]。
Nisoxetine 抑制[3H]去甲肾上腺素摄取到大鼠额叶皮质突触体中，Ki 为 2.1±0.3 nM[2]。
Nisoxetine 抑制 Na+ 电流，膜电位为 -70 和 -100 mV 时的 IC50 分别为 1.6 和 28.6 µM[3]。

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

Nisoxetine 相关抗体:
体内研究
(In Vivo)

Nisoxetine (2.2 µM; a single intrathecal injection) shows 100, 100, and 100% of blockades in motor function, proprioception, and with duration of action of about 61, 96, and 236 min, respectively[3].
Nisoxetine (3,10, 30 mg/kg, i.p.) inhibits refeeding response (intake of standard chow) in rats[4].

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

Animal Model: Sprague-Dawley rats(290-340 g)[3]
Dosage: 0.6, 1.2, 1.8, 2.2 µM
Administration: A single intrathecal injection
Result: Showed ED50s of 0.82, 0.75 and 0.70 µM in blocking motor function, proprioception, and nociception respectively.
分子量

271.35

Formula

C17H21NO2
CAS 号
性状

粘稠液体

颜色

Colorless to light yellow

中文名称

尼索西汀
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 250 mg/mL (921.32 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 3.6853 mL 18.4264 mL 36.8528 mL
5 mM 0.7371 mL 3.6853 mL 7.3706 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。-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
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Nisoxetine 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。-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 3.6853 mL 18.4264 mL 36.8528 mL 92.1319 mL
5 mM 0.7371 mL 3.6853 mL 7.3706 mL 18.4264 mL
10 mM 0.3685 mL 1.8426 mL 3.6853 mL 9.2132 mL
15 mM 0.2457 mL 1.2284 mL 2.4569 mL 6.1421 mL
20 mM 0.1843 mL 0.9213 mL 1.8426 mL 4.6066 mL
25 mM 0.1474 mL 0.7371 mL 1.4741 mL 3.6853 mL
30 mM 0.1228 mL 0.6142 mL 1.2284 mL 3.0711 mL
40 mM 0.0921 mL 0.4607 mL 0.9213 mL 2.3033 mL
50 mM 0.0737 mL 0.3685 mL 0.7371 mL 1.8426 mL
60 mM 0.0614 mL 0.3071 mL 0.6142 mL 1.5355 mL
80 mM 0.0461 mL 0.2303 mL 0.4607 mL 1.1516 mL
100 mM 0.0369 mL 0.1843 mL 0.3685 mL 0.9213 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:

Nisoxetine53179-07-0尼索西汀Monoamine TransporterSodium ChannelNa channelsNa+ channelsNoradrenalinetransporterNETantidepressantlocalanestheticsodiumchannelsuptakedepressionInhibitorinhibitorinhibit

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