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

Nisoxetine  (Synonyms: 尼索西汀)

目錄號: HY-B1704 純度: 98.28%
COA 產(chǎn)品使用指南

Nisoxetine 是一種有效的和選擇性的去甲腎上腺素轉(zhuǎn)運蛋白 (NET) 抑制劑，Kd 值為 0.76 nM。Nisoxetine 是一種抗抑郁試劑和局部麻藥，它可以阻斷電壓門控性鈉通道。

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Nisoxetine Chemical Structure

Nisoxetine Chemical Structure

CAS No. : 53179-07-0

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5 mg ￥950
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10 mg ￥1500
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25 mg ￥3000
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50 mg ￥4900
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Other Forms of Nisoxetine:

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

查看 Sodium Channel 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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]
細(xì)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]
體外研究
(In Vitro)

Nisoxetine 抑制 [3H]Nisoxetine 與大鼠額葉皮層膜的結(jié)合，Ki 為 1.4±0.1 nM[2]。
Nisoxetine 抑制[3H]去甲腎上腺素攝取到大鼠額葉皮質(zhì)突觸體中，Ki 為 2.1±0.3 nM[2]。
Nisoxetine 抑制 Na+ 電流，膜電位為 -70 和 -100 mV 時的 IC50 分別為 1.6 和 28.6 μM[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)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 號
性狀

粘稠液體

顏色

Colorless to light yellow

中文名稱

尼索西汀
運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實驗： 

DMSO 中的溶解度 : 250 mg/mL (921.32 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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.

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產(chǎn)品名稱：
Nisoxetine
目錄號：
HY-B1704
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