Art. -Nr.: HY-B1704

Nisoxetine

2 Cited Publications

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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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Reinheit: 98.56%
CAS. Nr.: 53179-07-0
Formel: C₁₇H₂₁NO₂
Molecular Weight:271.35

Speicherung:

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

Nisoxetine Chemical Structure

CAS. Nr.: 53179-07-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Kd: 0.76 nM (NET)^[1]

Alle Sodium Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
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	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	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 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]
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]
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.

Chemical Information

CAS. Nr. 53179-07-0
Appearance Viscous Liquid
Molecular Weight 271.35
Formel C₁₇H₂₁NO₂
Color Colorless to light yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (2)

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Journal Impact Factor

Cell Discov

TGM2-mediated serotonylation of GPX4 confers ferroptosis resistance to promote gastric tumorigenesis. [Abstract]

2026 Apr 28;12(1):30. PMID: 42049702
Crit Rev Anal Chem

A Critical Review on Advancement in Analytical Strategies for the Quantification of Clinically Relevant Biological Transporters. [Abstract]

2022;52(7):1557-1571. PMID: 33691566

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Nisoxetine

2 Cited Publications

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Nisoxetine

Neuroprotective Compound Library

Mechanoreceptors Compound Library

Antidepressant Compound Library

Sodium Channel Blocker Library

Human Metabolite Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Membrane Transporter/Ion Channel Compound Library

Publications Citing Use of MedChemExpress (MCE) Nisoxetine

Alle Sodium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Nisoxetine

Neuroprotective Compound Library

Mechanoreceptors Compound Library

Antidepressant Compound Library

Sodium Channel Blocker Library

Human Metabolite Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Membrane Transporter/Ion Channel Compound Library

Publications Citing Use of MedChemExpress (MCE) Nisoxetine

Alle Sodium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Nisoxetine Related Classifications

HY-B1704 Related Classifications