Nisoxetine hydrochloride
Based on 2 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.92%
- CAS No.: 57754-86-6
- Formula: C17H22ClNO2
- Molecular Weight:307.82
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Nisoxetine hydrochloride
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Biological Activity
Kd: 0.76 nM (NET)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.005 μM
Compound: Nisoxetine
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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
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[PMID: 34112854] |
| HEK293 | IC50 |
0.005 μM
Compound: Nisoxetine
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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 (PubChem AID: 174586
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 (PubChem AID: 174586
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[PMID: 34112854] |
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 (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.
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Animal Model:Sprague-Dawley rats(290-340 g)[3]
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Dosage:0.6, 1.2, 1.8, 2.2 µM
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Administration:A single intrathecal injection
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Result:Showed ED50s of 0.82, 0.75 and 0.70 µM in blocking motor function, proprioception, and nociception respectively.
Chemical Information
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CAS No. 57754-86-6
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Appearance Solid
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Molecular Weight 307.82
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Formula C17H22ClNO2
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Color White to off-white
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SMILES
CNCCC(OC1=CC=CC=C1OC)C2=CC=CC=C2.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -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
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Most Recent
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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
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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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
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.
Nisoxetine hydrochloride Related Classifications
HY-B1704A Related Classifications
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