Nisoxetine

Name: Nisoxetine
Brand: MedChemExpress
SKU: HY-B1704
Rating: 4.5 (1 reviews)

Cat. No.: HY-B1704 Pureza: 98.56%: Ficha de datos
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Nisoxetine is a potent and selective inhibitor of noradrenaline transporter (NET), with a K_d of 0.76 nM. Nisoxetine is an antidepressant and local anesthetic, it can block voltage-gated sodium channels.

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Nisoxetine Estructura química

No. CAS : 53179-07-0

Tamaño	Stock	Cantidad
Solid or liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
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5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

Other Forms of Nisoxetine:

Nisoxetine hydrochloride In-stock
Nisoxetine (Standard) Obtener un presupuesto

1 Publications Citing Use of MCE Nisoxetine

•Crit Rev Anal Chem. 2022;52(7):1557-1571. [Abstract]

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Sodium Channel:

Ver todas las isoformas

Na_v1.1 Na_v1.2 Na_v1.3 Na_v1.4 Na_v1.5 Na_v1.6 Na_v1.7 Na_v1.8 Na_v1.9

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Descripciòn

IC₅₀ & Target

Kd: 0.76 nM (NET)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
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	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 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	1400 nM Compound: 2	Inhibition of serotonin uptake at human SERT in human HEK293 cells Inhibition of serotonin uptake at human SERT in human HEK293 cells	[PMID: 18550369]
HEK293	IC₅₀	1400 nM Compound: Nisoxetine	Inhibition of serotonin uptake at human SERT expressed in HEK cells Inhibition of serotonin uptake at human SERT expressed in HEK cells	[PMID: 18667309]
HEK293	IC₅₀	15 nM Compound: 2	Inhibition of norepinephrine uptake at human NET in human HEK293 cells Inhibition of norepinephrine uptake at human NET in human HEK293 cells	[PMID: 18550369]
HEK293	IC₅₀	15 nM Compound: Nisoxetine	Inhibition of norepinephrine uptake at human NET expressed in HEK cells Inhibition of norepinephrine uptake at human NET expressed in HEK cells	[PMID: 18667309]
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 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	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	2400 nM Compound: 2	Inhibition of dopamine uptake at human DAT in human HEK293 cells Inhibition of dopamine uptake at human DAT in human HEK293 cells	[PMID: 18550369]
HEK293	IC₅₀	2400 nM Compound: Nisoxetine	Inhibition of dopamine uptake at human DAT expressed in HEK cells Inhibition of dopamine uptake at human DAT expressed in HEK cells	[PMID: 18667309]
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]
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 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]
JAR	IC₅₀	277 nM Compound: 5	Inhibition of serotonin uptake at human SERT expressed in JAR cells Inhibition of serotonin uptake at human SERT expressed in JAR cells	[PMID: 18771916]
MDCK	IC₅₀	6 nM Compound: 5	Inhibition of norepinephrine uptake at human NET expressed in MDCK cells Inhibition of norepinephrine uptake at human NET expressed in MDCK cells	[PMID: 18771916]
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]

In Vitro

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

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.

Peso molecular

271.35

Fòrmula

C₁₇H₂₁NO₂

No. CAS

53179-07-0

Appearance

Viscous Liquid

Color

Colorless to light yellow

SMILES

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

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvente y solubilidad

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
10 mM	0.3685 mL	1.8426 mL	3.6853 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.

Calculadora de molaridad
Calculadora de dilución

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

Concentration _(start)

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Concentration _(final)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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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

Pureza y Documentación

Purity: 98.56%

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Ficha de datos (276 KB) SDS (252 KB)

COA (250 KB) HNMR (259 KB) LCMS (98 KB)

Instrucciones de manejo (2659 KB)

Referencias

[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

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

Nisoxetine Related Classifications

Neurological Disease

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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Nisoxetine

Revisión del cliente

Other Forms of Nisoxetine:

Nisoxetine Related Antibodies

1 Publications Citing Use of MCE Nisoxetine

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Sodium Channel:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

Nisoxetine Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

Nisoxetine Related Classifications

Keywords:

Productos vistos recientemente:

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