1. Neuronal Signaling Membrane Transporter/Ion Channel
  2. Serotonin Transporter Sodium Channel
  3. Atomoxetine

Atomoxetine  (Synonyms: Tomoxetine; (R)-Tomoxetine)

Art. -Nr.: HY-107370 Reinheit: 98.50%
Handling Instructions Technical Support

Atomoxetine (Tomoxetine) is a selective noradrenaline reuptake inhibitor with Ki values of 5, 77 and 1451 nM for norepinephrine (NE), serotonin (5-HT) and dopamine (DA) transporters, respectively. Atomoxetine (Tomoxetine) increases of DAEX and NEEX in the PFC and enhances catecholaminergic neurotransmission. Atomoxetine (Tomoxetine) is a potent Na+ channels (VGSCs) blocker. Atomoxetine (Tomoxetine) can be used for attention-deficit hyperactivity disorder (ADHD) research.

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Atomoxetine

Atomoxetine Chemische Struktur

CAS. Nr. : 83015-26-3

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Oil + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
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Based on 4 publication(s) in Google Scholar

Other Forms of Atomoxetine:

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Beschreibung

Atomoxetine (Tomoxetine) is a selective noradrenaline reuptake inhibitor with Ki values of 5, 77 and 1451 nM for norepinephrine (NE), serotonin (5-HT) and dopamine (DA) transporters, respectively. Atomoxetine (Tomoxetine) increases of DAEX and NEEX in the PFC and enhances catecholaminergic neurotransmission. Atomoxetine (Tomoxetine) is a potent Na+ channels (VGSCs) blocker. Atomoxetine (Tomoxetine) can be used for attention-deficit hyperactivity disorder (ADHD) research[1][2][3].

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
190 1
Compound: 6
Displacement of [alpha,beta-3H(N)]-5-hydroxytryptamine from human cloned SERT expressed in HEK293 cells by microplate scintillation counter
Displacement of [alpha,beta-3H(N)]-5-hydroxytryptamine from human cloned SERT expressed in HEK293 cells by microplate scintillation counter
[PMID: 18954038]
MDCK IC50
3 1
Compound: 4
Inhibition of norepinephrine uptake at human NET expressed in MDCK cells
Inhibition of norepinephrine uptake at human NET expressed in MDCK cells
[PMID: 18771916]
HEK293 IC50
2.1 3
Compound: 6
Inhibition of human ERG expressed in HEK293 cells by patch-clamp method
Inhibition of human ERG expressed in HEK293 cells by patch-clamp method
[PMID: 18954038]
HEK293 IC50
5 1
Compound: 1
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
3100 1
Compound: 6
Displacement of 3,4-[ring-2,5,6-3H]dihydroxyphenylethylamine from human cloned DAT expressed in HEK293 cells by microplate scintillation counter
Displacement of 3,4-[ring-2,5,6-3H]dihydroxyphenylethylamine from human cloned DAT expressed in HEK293 cells by microplate scintillation counter
[PMID: 18954038]
HEK293 IC50
180 1
Compound: 1
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
5 1
Compound: atomoxetine
Inhibition of norepinephrine uptake at human NET expressed in HEK293 cells
Inhibition of norepinephrine uptake at human NET expressed in HEK293 cells
[PMID: 18672364]
HEK293 IC50
180 1
Compound: 1
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
5.1 1
Compound: 6
Displacement of Levo[ring-2,5,6-3H]norepinephrine from human cloned NET expressed in HEK293 cells by microplate scintillation counter
Displacement of Levo[ring-2,5,6-3H]norepinephrine from human cloned NET expressed in HEK293 cells by microplate scintillation counter
[PMID: 18954038]
HEK293 IC50
5 1
Compound: 1
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
5 1
Compound: atomoxetine
Inhibition of norepinephrine uptake at human NET transfected in HEK cells
Inhibition of norepinephrine uptake at human NET transfected in HEK cells
[PMID: 18954981]
HeLa IC50
100 3
Compound: Atomoxetine
Inhibition of human KLF10 expressed in human HeLa cells assessed as reduction in transcriptional activity after 24 hrs by CACCC-responsive promoter driven TK-luciferase reporter gene assay
Inhibition of human KLF10 expressed in human HeLa cells assessed as reduction in transcriptional activity after 24 hrs by CACCC-responsive promoter driven TK-luciferase reporter gene assay
[PMID: 25581017]
HEK293 IC50
180 1
Compound: atomoxetine
Inhibition of serotonin uptake at human SERT expressed in HEK293 cells
Inhibition of serotonin uptake at human SERT expressed in HEK293 cells
[PMID: 18672364]
HEK293 IC50
180 1
Compound: atomoxetine
Inhibition of serotonin uptake at human SERT transfected in HEK cells
Inhibition of serotonin uptake at human SERT transfected in HEK cells
[PMID: 18954981]
HEK293 IC50
5.1 1
Compound: 6
Displacement of Levo[ring-2,5,6-3H]norepinephrine from human cloned NET expressed in HEK293 cells by microplate scintillation counter
Displacement of Levo[ring-2,5,6-3H]norepinephrine from human cloned NET expressed in HEK293 cells by microplate scintillation counter
[PMID: 18954038]
HEK293 IC50
3 3
Compound: 1
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
190 1
Compound: 6
Displacement of [alpha,beta-3H(N)]-5-hydroxytryptamine from human cloned SERT expressed in HEK293 cells by microplate scintillation counter
Displacement of [alpha,beta-3H(N)]-5-hydroxytryptamine from human cloned SERT expressed in HEK293 cells by microplate scintillation counter
[PMID: 18954038]
HEK293 IC50
3 3
Compound: atomoxetine
Inhibition of dopamine uptake at human DAT expressed in HEK293 cells
Inhibition of dopamine uptake at human DAT expressed in HEK293 cells
[PMID: 18672364]
HEK293 IC50
2.1 3
Compound: 6
Inhibition of human ERG expressed in HEK293 cells by patch-clamp method
Inhibition of human ERG expressed in HEK293 cells by patch-clamp method
[PMID: 18954038]
HEK293 IC50
3 3
Compound: 1
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
3000 1
Compound: 1
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
3 3
Compound: atomoxetine
Inhibition of dopamine uptake at human DAT transfected in HEK cells
Inhibition of dopamine uptake at human DAT transfected in HEK cells
[PMID: 18954981]
HEK293 IC50
3000 1
Compound: 1
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
3000 1
Compound: atomoxetine
Inhibition of dopamine uptake at human DAT expressed in HEK293 cells
Inhibition of dopamine uptake at human DAT expressed in HEK293 cells
[PMID: 18672364]
HEK293 IC50
2.1 3
Compound: 6
Inhibition of human ERG expressed in HEK293 cells by patch-clamp method
Inhibition of human ERG expressed in HEK293 cells by patch-clamp method
[PMID: 18954038]
HEK293 IC50
>5 3
Compound: 6 (Atomoxetine)
Inhibitory activity against Opioid receptor delta 1 expressed in HEK293 cells
Inhibitory activity against Opioid receptor delta 1 expressed in HEK293 cells
[PMID: 15225731]
HEK293 IC50
3000 1
Compound: atomoxetine
Inhibition of dopamine uptake at human DAT transfected in HEK cells
Inhibition of dopamine uptake at human DAT transfected in HEK cells
[PMID: 18954981]
HEK293 IC50
3100 1
Compound: 6
Displacement of 3,4-[ring-2,5,6-3H]dihydroxyphenylethylamine from human cloned DAT expressed in HEK293 cells by microplate scintillation counter
Displacement of 3,4-[ring-2,5,6-3H]dihydroxyphenylethylamine from human cloned DAT expressed in HEK293 cells by microplate scintillation counter
[PMID: 18954038]
HeLa IC50
100 3
Compound: Atomoxetine
Inhibition of human KLF10 expressed in human HeLa cells assessed as reduction in transcriptional activity after 24 hrs by CACCC-responsive promoter driven TK-luciferase reporter gene assay
Inhibition of human KLF10 expressed in human HeLa cells assessed as reduction in transcriptional activity after 24 hrs by CACCC-responsive promoter driven TK-luciferase reporter gene assay
[PMID: 25581017]
HEK293 IC50
4186 1
Compound: 6 (Atomoxetine)
Inhibitory activity against Opioid receptor mu 1 expressed in HEK293 cells
Inhibitory activity against Opioid receptor mu 1 expressed in HEK293 cells
[PMID: 15225731]
JAR IC50
48 1
Compound: 2
Inhibition of serotonin uptake at human SERT expressed in human JAR cells
Inhibition of serotonin uptake at human SERT expressed in human JAR cells
[PMID: 19329313]
HEK293 IC50
4383 1
Compound: 6 (Atomoxetine)
Inhibitory activity against Opioid receptor kappa 1 expressed in HEK293 cells
Inhibitory activity against Opioid receptor kappa 1 expressed in HEK293 cells
[PMID: 15225731]
JAR IC50
48 1
Compound: 4
Inhibition of serotonin uptake at human SERT expressed in JAR cells
Inhibition of serotonin uptake at human SERT expressed in JAR cells
[PMID: 18771916]
JAR IC50
48 1
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: 18951020]
HEK293 IC50
5 1
Compound: 1
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
5 1
Compound: 1
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
180 1
Compound: 1
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
180 1
Compound: atomoxetine
Inhibition of serotonin uptake at human SERT expressed in HEK293 cells
Inhibition of serotonin uptake at human SERT expressed in HEK293 cells
[PMID: 18672364]
HEK293 IC50
5 1
Compound: atomoxetine
Inhibition of norepinephrine uptake at human NET expressed in HEK293 cells
Inhibition of norepinephrine uptake at human NET expressed in HEK293 cells
[PMID: 18672364]
HEK293 IC50
5 1
Compound: atomoxetine
Inhibition of norepinephrine uptake at human NET transfected in HEK cells
Inhibition of norepinephrine uptake at human NET transfected in HEK cells
[PMID: 18954981]
HEK293 IC50
180 1
Compound: 1
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
180 1
Compound: atomoxetine
Inhibition of serotonin uptake at human SERT transfected in HEK cells
Inhibition of serotonin uptake at human SERT transfected in HEK cells
[PMID: 18954981]
HEK293 IC50
5.1 1
Compound: 6
Displacement of Levo[ring-2,5,6-3H]norepinephrine from human cloned NET expressed in HEK293 cells by microplate scintillation counter
Displacement of Levo[ring-2,5,6-3H]norepinephrine from human cloned NET expressed in HEK293 cells by microplate scintillation counter
[PMID: 18954038]
HEK293 IC50
190 1
Compound: 6
Displacement of [alpha,beta-3H(N)]-5-hydroxytryptamine from human cloned SERT expressed in HEK293 cells by microplate scintillation counter
Displacement of [alpha,beta-3H(N)]-5-hydroxytryptamine from human cloned SERT expressed in HEK293 cells by microplate scintillation counter
[PMID: 18954038]
HEK293 IC50
> 5000 1
Compound: 6 (Atomoxetine)
Inhibitory activity against Opioid receptor delta 1 expressed in HEK293 cells
Inhibitory activity against Opioid receptor delta 1 expressed in HEK293 cells
[PMID: 15225731]
HEK293 IC50
> 5000 1
Compound: 6 (Atomoxetine)
Inhibitory activity against Opioid receptor like 1 expressed in HEK293 cells
Inhibitory activity against Opioid receptor like 1 expressed in HEK293 cells
[PMID: 15225731]
HEK293 IC50
3100 1
Compound: 6
Displacement of 3,4-[ring-2,5,6-3H]dihydroxyphenylethylamine from human cloned DAT expressed in HEK293 cells by microplate scintillation counter
Displacement of 3,4-[ring-2,5,6-3H]dihydroxyphenylethylamine from human cloned DAT expressed in HEK293 cells by microplate scintillation counter
[PMID: 18954038]
HEK293 IC50
4186 1
Compound: 6 (Atomoxetine)
Inhibitory activity against Opioid receptor mu 1 expressed in HEK293 cells
Inhibitory activity against Opioid receptor mu 1 expressed in HEK293 cells
[PMID: 15225731]
HEK293 IC50
4383 1
Compound: 6 (Atomoxetine)
Inhibitory activity against Opioid receptor kappa 1 expressed in HEK293 cells
Inhibitory activity against Opioid receptor kappa 1 expressed in HEK293 cells
[PMID: 15225731]
HeLa IC50
100 3
Compound: Atomoxetine
Inhibition of human KLF10 expressed in human HeLa cells assessed as reduction in transcriptional activity after 24 hrs by CACCC-responsive promoter driven TK-luciferase reporter gene assay
Inhibition of human KLF10 expressed in human HeLa cells assessed as reduction in transcriptional activity after 24 hrs by CACCC-responsive promoter driven TK-luciferase reporter gene assay
[PMID: 25581017]
JAR IC50
48 1
Compound: 2
Inhibition of serotonin uptake at human SERT expressed in human JAR cells
Inhibition of serotonin uptake at human SERT expressed in human JAR cells
[PMID: 19329313]
JAR IC50
48 1
Compound: 4
Inhibition of serotonin uptake at human SERT expressed in JAR cells
Inhibition of serotonin uptake at human SERT expressed in JAR cells
[PMID: 18771916]
JAR IC50
48 1
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: 18951020]
MDCK IC50
3 1
Compound: 4
Inhibition of norepinephrine uptake at human NET expressed in MDCK cells
Inhibition of norepinephrine uptake at human NET expressed in MDCK cells
[PMID: 18771916]
In Vitro

Atomoxetine (Tomoxetine) (1-100 μM; 0.5-20 seconds; tsA201 cells) interacts with the human heart muscle sodium channel (hNav1.5) in a state and dose-dependent manner[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Atomoxetine (Tomoxetine) (0.3-3 mg/kg; i.p.; 0-4 hours; male Sprague-Dawley rats) increases extracellular norepinephrine and dopamine by 3-fold and increases Fos expression in the rat prefrontal cortex[1].
Atomoxetine (Tomoxetine) (0.1-5 mg/kg; i.p. and p.o; for 14 days; spontaneously hypertensive rat) can improve behaviors associated with ADHD in rats[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats[1]
Dosage: 0.3, 1 and 3 mg/kg
Administration: Intraperitoneal injection; for 4 hours
Result: Increased the number of cells expressing Fos-like immunoreactivity in PFC 3.7-fold and increased extracellular norepinephrine and dopamine by 3-fold.
Animal Model: Spontaneously hypertensive rat (SHR)[3]
Dosage: 0.1, 0.3, 1.25 and 5.0 mg/kg
Administration: Intraperitoneal injection and oral administration; for 14 days
Result: Had non-impact on the measurement of motor activity.
Klinische Studie
Molekulargewicht

255.35

Formel

C17H21NO

CAS. Nr.
Appearance

Oil

Color

Colorless to light yellow

SMILES

CC(C=CC=C1)=C1O[C@@H](C2=CC=CC=C2)CCNC

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
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 100 mg/mL (391.62 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 3.9162 mL 19.5810 mL 39.1619 mL
5 mM 0.7832 mL 3.9162 mL 7.8324 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.

  • Molaritätsrechner

  • Verdünnungsrechner

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
Verweise

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
DMSO 1 mM 3.9162 mL 19.5810 mL 39.1619 mL 97.9048 mL
5 mM 0.7832 mL 3.9162 mL 7.8324 mL 19.5810 mL
10 mM 0.3916 mL 1.9581 mL 3.9162 mL 9.7905 mL
15 mM 0.2611 mL 1.3054 mL 2.6108 mL 6.5270 mL
20 mM 0.1958 mL 0.9790 mL 1.9581 mL 4.8952 mL
25 mM 0.1566 mL 0.7832 mL 1.5665 mL 3.9162 mL
30 mM 0.1305 mL 0.6527 mL 1.3054 mL 3.2635 mL
40 mM 0.0979 mL 0.4895 mL 0.9790 mL 2.4476 mL
50 mM 0.0783 mL 0.3916 mL 0.7832 mL 1.9581 mL
60 mM 0.0653 mL 0.3263 mL 0.6527 mL 1.6317 mL
80 mM 0.0490 mL 0.2448 mL 0.4895 mL 1.2238 mL
100 mM 0.0392 mL 0.1958 mL 0.3916 mL 0.9790 mL
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