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

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.

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Nisoxetine Chemical Structure

Nisoxetine Chemical Structure

CAS No. : 53179-07-0

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Other Forms of Nisoxetine:

Nisoxetine Related Antibodies

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  • Purity & Documentation

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  • Customer Review

Description

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]
In Vitro

Nisoxetine inhibits [3H]Nisoxetine binding to rat frontal cortical membranes with a Ki of 1.4±0.1 nM[2].
Nisoxetine inhibits [3H]Noradrenaline uptake into rat frontal cortical synaptosomes with a Ki of 2.1±0.3 nM[2].
Nisoxetine inhibits Na+ currents with IC50s of 1.6 and 28.6 µM at the membrane potential of -70 and -100 mV, respectively[3].

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

Nisoxetine Related Antibodies
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].

MedChemExpress (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.
Molecular Weight

271.35

Formula

C17H21NO2
CAS No.
Appearance

Viscous Liquid

Color

Colorless to light yellow

SMILES

CNCCC(OC1=CC=CC=C1OC)C2=CC=CC=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (921.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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Nisoxetine Related Classifications

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:

Nisoxetine53179-07-0Monoamine TransporterSodium ChannelNa channelsNa+ channelsNoradrenalinetransporterNETantidepressantlocalanestheticsodiumchannelsuptakedepressionInhibitorinhibitorinhibit

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