Nisoxetine hydrochloride

Name: Nisoxetine hydrochloride
Brand: MedChemExpress
SKU: HY-B1704A
Rating: 4.5 (1 reviews)

Cat. No.: HY-B1704A Purity: 99.81%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

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

For research use only. We do not sell to patients.

Nisoxetine hydrochloride Chemical Structure

CAS No. : 57754-86-6

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Nisoxetine hydrochloride:

Nisoxetine Get quote

1 Publications Citing Use of MCE Nisoxetine hydrochloride

•Crit Rev Anal Chem. 2021 Mar 10;1-15. [Abstract]

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•Related Screening Libraries:

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View All Sodium Channel Isoform Specific Products:

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Na_v1.1 Na_v1.2 Na_v1.3 Na_v1.4 Na_v1.5 Na_v1.6 Na_v1.7 Na_v1.8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Kd: 0.76 nM (NET)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.005 μM Compound: Nisoxetine	Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells	[PMID: 34112854]

In Vitro

Nisoxetine hydrochloride inhibits [³H]Nisoxetine binding to rat frontal cortical membranes with a K_i of 1.4±0.1 nM^[2].
Nisoxetine hydrochloride inhibits [³H]Noradrenaline uptake into rat frontal cortical synaptosomes with a K_i 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.

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.

57754-86-6

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
10 mM	0.3249 mL	1.6243 mL	3.2487 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg

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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%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (251 KB) HNMR (281 KB) LCMS (260 KB)

Handling Instructions (2659 KB)

References

[1]. Béïque JC, et, al. Affinities of venlafaxine and various reuptake inhibitors for the serotonin and norepinephrine transporters. Eur J Pharmacol. 1998 May 15; 349(1): 129-32. [Content Brief]

[2]. Cheetham SC, et, al. [3H]nisoxetine-a radioligand for noradrenaline reuptake sites: correlation with inhibition of [3H]noradrenaline uptake and effect of DSP-4 lesioning and antidepressant treatments. Neuropharmacology. 1996 Jan; 35(1): 63-70. [Content Brief]

[3]. Leung YM, et, al. Nisoxetine blocks sodium currents and elicits spinal anesthesia in rats. Pharmacol Rep. 2013; 65(2): 350-7. [Content Brief]

[4]. Bello NT, et al. High-fat diet-induced alterations in the feeding suppression of low-dose nisoxetine, a selective norepinephrine reuptake inhibitor. J Obes. 2013;2013:457047. [Content Brief]

Complete Stock Solution Preparation Table

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.