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Nisoxetine

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Catalog No. T69145Cas No. 53179-07-0

Nisoxetine is a selective NET (noradrenaline transporter) inhibitor (Kd=0.76 nM) capable of blocking voltage-gated sodium channels, inducing spinal anaesthesia in rats, and exhibiting antidepressant effects.

Nisoxetine

Nisoxetine

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Purity: 98.71%
Catalog No. T69145Cas No. 53179-07-0
Nisoxetine is a selective NET (noradrenaline transporter) inhibitor (Kd=0.76 nM) capable of blocking voltage-gated sodium channels, inducing spinal anaesthesia in rats, and exhibiting antidepressant effects.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$34-In Stock
5 mg$77-In Stock
10 mg$123-In Stock
25 mg$247-In Stock
50 mg$396-In Stock
100 mg$648-In Stock
200 mg$892-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:98.71%
Appearance:Oil
Color:Brown
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Product Introduction

Bioactivity
Description
Nisoxetine is a selective NET (noradrenaline transporter) inhibitor (Kd=0.76 nM) capable of blocking voltage-gated sodium channels, inducing spinal anaesthesia in rats, and exhibiting antidepressant effects.
Targets&IC50
NET:0.76 nM (Kd)
In vitro
Nisoxetine inhibits the binding of [3H]Nisoxetine on rat frontal cortex membranes with a Ki = 1.4 ± 0.1 nM[2].
Nisoxetine inhibits the uptake of [3H]norepinephrine in rat frontal cortex synaptosomes with a Ki = 2.1 ± 0.3 nM[2].
At membrane potentials of -70 mV and -100 mV, the IC50 values of Nisoxetine for Na+ currents are 1.6 μM and 28.6 μM, respectively[3].
In vivo
Acute administration of Nisoxetine (saline: 0, 3, 10, and 30 mg/kg; i.p.) resulted in a dose-dependent reduction in the 24 h refeeding response in male Sprague Dawley rats maintained on standard chow [4].
Chemical Properties
Molecular Weight271.35
FormulaC17H21NO2
Cas No.53179-07-0
SmilesO(C=1C=CC=CC1OC(C=2C=CC=CC2)CCNC)C
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 200 mg/mL (737.06 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.6853 mL18.4264 mL36.8528 mL184.2639 mL
5 mM0.7371 mL3.6853 mL7.3706 mL36.8528 mL
10 mM0.3685 mL1.8426 mL3.6853 mL18.4264 mL
20 mM0.1843 mL0.9213 mL1.8426 mL9.2132 mL
50 mM0.0737 mL0.3685 mL0.7371 mL3.6853 mL
100 mM0.0369 mL0.1843 mL0.3685 mL1.8426 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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%
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Keywords

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