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Atomoxetine HCl 5-HT Receptor inhibitor

Name: Atomoxetine HCl
Brand: Selleck Chemicals
SKU: S3175
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S3175

Atomoxetine (LY 139603) is a selective norepinephrine (NE) transporter inhibitor with K_i of 5 nM, with 15- and 290-fold lower affinity for human 5-HT and DA transporters.

Chemical Structure

Molecular Weight: 291.82

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S317501 DMSO]58 mg/mL]false]Ethanol]37 mg/mL]false]Water]2 mg/mL]false Purity: 99.96%

99.96

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Chemical Information, Storage & Stability

Molecular Weight	291.82	Formula	C₁₇H₂₁NO.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	82248-59-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	LY 139603 HCl			Smiles	CC1=CC=CC=C1OC(CCNC)C2=CC=CC=C2.Cl

Solubility

In vitro
Batch:

DMSO : 58 mg/mL (198.75 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 37 mg/mL

Water : 2 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.9mg/ml (9.94mM)	Taking the 1 mL working solution as an example, add 50 μL of 58 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.41mg/ml (1.40mM)	Taking the 1 mL working solution as an example, add 50 μL of 8.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Norepinephrine (NE) transporter ^[1] 5 nM(Ki) 5-HT ^[1] 77 nM(Ki) DA transporter ^[1] 1451 nM(Ki)
In vitro	Atomoxetine is a selective norepinephrine reuptake inhibitor with K_i of 5 nM, compared with 77 and 1451 nM for binding to serotonin and dopamine transporters. ^[1]
In vivo	In microdialysis studies, atomoxetine increases extracellular (EX) levels of NE in prefrontal cortex (PFC) 3-fold, but does not alter 5-HT_EX levels. Atomoxetine also increases DA_EX concentrations in PFC 3-fold, but does not alter DA_EX in striatum or nucleus accumbens. Atomoxetine increases Fos by 3.7-fold in PFC, but not in the striatum or nucleus accumbens. ^[1] Atomoxetine selectively inhibits the presynaptic uptake of norepinephrine in adrenergic neurons in animals, and has activity in animal models of depression. ^[2]^[3]
References	[1] https://pubmed.ncbi.nlm.nih.gov/12431845/ [2] https://pubmed.ncbi.nlm.nih.gov/3965689/ [3] https://pubmed.ncbi.nlm.nih.gov/6123593/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03154359	Completed	ADHD	Children''s Mercy Hospital Kansas City\|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)	December 12 2017	--
NCT03460210	Recruiting	Obesity Morbid	Norwegian University of Science and Technology\|St. Olavs Hospital\|Volvat Medisinsk Senter Stokkan\|Namsos Hospital\|Alesund Hospital	November 2 2016	--
NCT01522404	Completed	Mild Cognitive Impairment	Emory University\|National Institute on Aging (NIA)	March 2012	Phase 2
NCT01709695	Completed	ADHD\|Attention Deficit Hyperactivity Disorder	Icahn School of Medicine at Mount Sinai	March 2011	Phase 4

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