Nisoxetine HCl | CAS# 57754-86-6 | NET inhibitor

MedKoo Cat#: 574813 | Name: Nisoxetine HCl

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Nisoxetine is a norepinephrine transporter (NET) inhibitor that inhibits norepinephrine uptake and inhibits amphetamine-induced increases in norepinephrine release. It reduces increases in locomotor activity induced by d-N-ethylamphetamine, methylphenidate, and cocaine, but not morphine and also reduces cataplexy in narcoleptic dogs.

Chemical Structure

Nisoxetine HCl

CAS#57754-86-6 (HCl)

Theoretical Analysis

MedKoo Cat#: 574813

Name: Nisoxetine HCl

CAS#: 57754-86-6 (HCl)

Chemical Formula: C17H22ClNO2

Exact Mass: 0.0000

Molecular Weight: 307.82

Elemental Analysis: C, 66.33; H, 7.20; Cl, 11.52; N, 4.55; O, 10.40

Price and Availability

Size	Price	Availability
50mg	USD 550.00	2 Weeks
100mg	USD 950.00	2 Weeks
200mg	USD 1,450.00	2 Weeks
500mg	USD 2,850.00	2 Weeks
1g	USD 4,250.00	2 Weeks
2g	USD 6,450.00	2 Weeks

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Related CAS #

53179-07-0 (free base) 57754-86-6 (HCl) 163059-33-4 (R-isomer)

Synonym

Lilly 94939; Lilly-94939; Lilly94939; NSC 298819; NSC-298819; NSC298819; Nisoxetine hydrochloride; Nisoxetine HCl;

IUPAC/Chemical Name

3-(2-methoxyphenoxy)-N-methyl-3-phenylpropan-1-amine hydrochloride

InChi Key

LCEURBZEQJZUPV-UHFFFAOYSA-N

InChi Code

InChI=1S/C17H21NO2.ClH/c1-18-13-12-15(14-8-4-3-5-9-14)20-17-11-7-6-10-16(17)19-2;/h3-11,15,18H,12-13H2,1-2H3;1H

SMILES Code

CNCCC(C1=CC=CC=C1)OC2=C(OC)C=CC=C2.Cl

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Nisoxetine hydrochloride is a potent and selective inhibitor of noradrenaline transporter (NET), with a Kd of 0.76 nM.

In vitro activity:

In in vitro studies, the voltage-clamp method was employed to examine whether nisoxetine blocked Na(+) currents in mouse neuroblastoma N2A cells. Nisoxetine was more potent (IC50 of 1.6 and 28.6 μM at holding potentials of -70 and -100 mV, respectively). Reference: Pharmacol Rep. 2013;65(2):350-7. https://pubmed.ncbi.nlm.nih.gov/23744419/

In vivo activity:

Acute administration of nisoxetine (saline: 0, 3, 10, and 30 mg/kg; i.p.) resulted in a dose-dependent reduction in the 24 h refeeding response in male Sprague Dawley rats maintained on standard chow. In a similar fashion, nisoxetine resulted in reductions in blood pressure and a compensatory increase in heart rate. Nisoxetine (3 mg/kg) also resulted in greater neural activation, as measured by c-Fos immunohistochemistry, in the arcuate nucleus of the hypothalamus in animals exposed to the high-fat diet. Reference: J Obes. 2013;2013:457047. https://pubmed.ncbi.nlm.nih.gov/23431425/

	Solvent	mg/mL	mM
Solubility
	DMSO	250.0	812.17
	Ethanol	50.0	162.43
	Water	19.6	63.53

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 307.82 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Leung YM, Chu CC, Kuo CS, Chen YW, Wang JJ. Nisoxetine blocks sodium currents and elicits spinal anesthesia in rats. Pharmacol Rep. 2013;65(2):350-7. doi: 10.1016/s1734-1140(13)71010-7. PMID: 23744419. 2. Bello NT, Walters AL, Verpeut JL, Cunha PP. High-fat diet-induced alterations in the feeding suppression of low-dose nisoxetine, a selective norepinephrine reuptake inhibitor. J Obes. 2013;2013:457047. doi: 10.1155/2013/457047. Epub 2013 Jan 30. PMID: 23431425; PMCID: PMC3570928. 3. Di Benedetto M, Feliciani D, D'Addario C, Izenwasser S, Candeletti S, Romualdi P. Effects of the selective norepinephrine uptake inhibitor nisoxetine on prodynorphin gene expression in rat CNS. Brain Res Mol Brain Res. 2004 Aug 23;127(1-2):115-20. doi: 10.1016/j.molbrainres.2004.05.011. PMID: 15306127.

In vitro protocol:

In vivo protocol:

1. Bello NT, Walters AL, Verpeut JL, Cunha PP. High-fat diet-induced alterations in the feeding suppression of low-dose nisoxetine, a selective norepinephrine reuptake inhibitor. J Obes. 2013;2013:457047. doi: 10.1155/2013/457047. Epub 2013 Jan 30. PMID: 23431425; PMCID: PMC3570928. 2. Di Benedetto M, Feliciani D, D'Addario C, Izenwasser S, Candeletti S, Romualdi P. Effects of the selective norepinephrine uptake inhibitor nisoxetine on prodynorphin gene expression in rat CNS. Brain Res Mol Brain Res. 2004 Aug 23;127(1-2):115-20. doi: 10.1016/j.molbrainres.2004.05.011. PMID: 15306127.

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PMID: 35989453; PMCID: PMC9613606. 10: Al-Khrasani M, Karadi DA, Galambos AR, Sperlagh B, Vizi ES. The Pharmacological Effects of Phenylephrine are Indirect, Mediated by Noradrenaline Release from the Cytoplasm. Neurochem Res. 2022 Nov;47(11):3272-3284. doi: 10.1007/s11064-022-03681-2. Epub 2022 Aug 9. PMID: 35945308; PMCID: PMC9546997. 11: Camacho-Hernandez GA, Casiraghi A, Rudin D, Luethi D, Ku TC, Guthrie DA, Straniero V, Valoti E, Schütz GJ, Sitte HH, Newman AH. Illuminating the norepinephrine transporter: fluorescent probes based on nisoxetine and talopram. RSC Med Chem. 2021 Jun 9;12(7):1174-1186. doi: 10.1039/d1md00072a. PMID: 34355183; PMCID: PMC8292982. 12: Sijben HJ, van Oostveen WM, Hartog PBR, Stucchi L, Rossignoli A, Maresca G, Scarabottolo L, IJzerman AP, Heitman LH. Label-free high-throughput screening assay for the identification of norepinephrine transporter (NET/SLC6A2) inhibitors. Sci Rep. 2021 Jun 10;11(1):12290. doi: 10.1038/s41598-021-91700-7. 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