2. Nisoxetine hydrochloride

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

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Nisoxetine hydrochloride Chemical Structure

Nisoxetine hydrochloride Chemical Structure

CAS No. : 57754-86-6

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 88 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Nisoxetine hydrochloride:

Nisoxetine hydrochloride Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Nisoxetine hydrochloride

  • Biological Activity

  • Purity & Documentation

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Description

Nisoxetine hydrochloride is a potent and selective inhibitor of noradrenaline transporter (NET), with a Kd of 0.76 nM. Nisoxetine hydrochloride 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 hydrochloride inhibits [3H]Nisoxetine binding to rat frontal cortical membranes with a Ki of 1.4±0.1 nM[2].
Nisoxetine hydrochloride inhibits [3H]Noradrenaline uptake into rat frontal cortical synaptosomes with a Ki of 2.1±0.3 nM[2].
Nisoxetine hydrochloride 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 hydrochloride Related Antibodies
In Vivo

Nisoxetine (2.2 µM; a single intrathecal injection) hydrochloride 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.) hydrochloride 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

307.82

Formula

C17H22ClNO2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CNCCC(OC1=CC=CC=C1OC)C2=CC=CC=C2.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -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 (812.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 8.33 mg/mL (27.06 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2487 mL 16.2433 mL 32.4865 mL
5 mM 0.6497 mL 3.2487 mL 6.4973 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.81%

COA (251 KB) HNMR (281 KB) LCMS (259 KB)

Handling Instructions (2659 KB)

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
H2O / DMSO 1 mM 3.2487 mL 16.2433 mL 32.4865 mL 81.2163 mL
5 mM 0.6497 mL 3.2487 mL 6.4973 mL 16.2433 mL
10 mM 0.3249 mL 1.6243 mL 3.2487 mL 8.1216 mL
15 mM 0.2166 mL 1.0829 mL 2.1658 mL 5.4144 mL
20 mM 0.1624 mL 0.8122 mL 1.6243 mL 4.0608 mL
25 mM 0.1299 mL 0.6497 mL 1.2995 mL 3.2487 mL
DMSO 30 mM 0.1083 mL 0.5414 mL 1.0829 mL 2.7072 mL
40 mM 0.0812 mL 0.4061 mL 0.8122 mL 2.0304 mL
50 mM 0.0650 mL 0.3249 mL 0.6497 mL 1.6243 mL
60 mM 0.0541 mL 0.2707 mL 0.5414 mL 1.3536 mL
80 mM 0.0406 mL 0.2030 mL 0.4061 mL 1.0152 mL
100 mM 0.0325 mL 0.1624 mL 0.3249 mL 0.8122 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • 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:

Nisoxetine57754-86-6Inhibitorinhibitorinhibit

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