1. Neuronal Signaling
  2. Serotonin Transporter
  3. Duloxetine

Duloxetine is a serotonin-norepinephrine reuptake inhibitor with a Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD).

For research use only. We do not sell to patients.

CAS No. : 116539-59-4

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Customer Review

Based on 12 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Duloxetine purchased from MedChemExpress. Usage Cited in: Autophagy. 2026 Mar 5.  [Abstract]

    Duloxetine hydrochloride (Duloxetine Hcl; 10 μM; 15 h) increased LC3-II levels incubated neurons in a nutrient-limited medium (nutrient deprivation, ND).

    Duloxetine purchased from MedChemExpress. Usage Cited in: Autophagy. 2026 Mar 5.  [Abstract]

    Duloxetine hydrochloride (Dulox.; 10 μM; 15 h) showed the average number of LAMP1+ puncta did not change in response to these treatments, we observed a significant swelling of LAMP1+ vesicles in Neuro-2a cells.

    Duloxetine purchased from MedChemExpress. Usage Cited in: Autophagy. 2026 Mar 5.  [Abstract]

    Duloxetine hydrochloride (Dulox.; 10 μM; 15 h) induced enlargement of the lysosome in Neuro-2a cells.

    Duloxetine purchased from MedChemExpress. Usage Cited in: Neurotox Res. 2020 Dec;38(4):859-870.  [Abstract]

    Duloxetine hydrochloride (Duloxetine; 0-100 μM; 24 h) inhibited cell viability in N2a cells (a) and C17.2 cells (b).

    Duloxetine purchased from MedChemExpress. Usage Cited in: Neurotox Res. 2020 Dec;38(4):859-870.  [Abstract]

    Duloxetine hydrochloride (Duloxetine; 0, 12.5, 25, 50, 100 μM; 24 h) inhibited N2a cells and C17.2 cells viability in a dose-dependent manner.

    Duloxetine purchased from MedChemExpress. Usage Cited in: Neurotox Res. 2020 Dec;38(4):859-870.  [Abstract]

    Duloxetine hydrochloride (Duloxetine; 0, 12.5, 25, 50, 100 μM; 24 h) inhibited N2a viability in a dose-dependent manner.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Duloxetine is a serotonin-norepinephrine reuptake inhibitor with a Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD)[1][2].

    Cellular Effect
    Cell Line Type Value Description References
    CHO IC50
    >1000 nM
    Compound: 2
    Displacement of [3H]WIN-35428 form human DAT expressed in CHO cell membranes
    Displacement of [3H]WIN-35428 form human DAT expressed in CHO cell membranes
    [PMID: 20378347]
    CHO IC50
    2.8 μM
    Compound: duloxetine
    Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
    Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
    [PMID: 23812503]
    HEK293 IC50
    19 nM
    Compound: duloxetine
    Inhibition of [3H]NA uptake at NA transporter expressed in HEK293 cells
    Inhibition of [3H]NA uptake at NA transporter expressed in HEK293 cells
    [PMID: 16750359]
    HEK293 IC50
    6 nM
    Compound: duloxetine
    Inhibition of [3H]5-HT uptake at 5HT transporter expressed in HEK293 cells
    Inhibition of [3H]5-HT uptake at 5HT transporter expressed in HEK293 cells
    [PMID: 16750359]
    HEK293 IC50
    870 nM
    Compound: duloxetine
    Inhibition of DA transporter expressed in HEK293 cells
    Inhibition of DA transporter expressed in HEK293 cells
    [PMID: 16750359]
    HEK293 IC50
    19 nM
    Compound: duloxetine
    Inhibition of [3H]NA reuptake at NA transporter in HEK293 cells
    Inhibition of [3H]NA reuptake at NA transporter in HEK293 cells
    [PMID: 16750363]
    HEK293 IC50
    6 nM
    Compound: duloxetine
    Inhibition of [3H]5-HT reuptake at 5HT transporter in HEK293 cells
    Inhibition of [3H]5-HT reuptake at 5HT transporter in HEK293 cells
    [PMID: 16750363]
    HEK293 IC50
    870 nM
    Compound: duloxetine
    Inhibition of [3H]DA reuptake at DA transporter in HEK293 cells
    Inhibition of [3H]DA reuptake at DA transporter in HEK293 cells
    [PMID: 16750363]
    HEK293 IC50
    19 nM
    Compound: duloxetine
    Inhibition of [3H]NA from human NET expressed in HEK293 cells
    Inhibition of [3H]NA from human NET expressed in HEK293 cells
    [PMID: 17267217]
    HEK293 IC50
    6 nM
    Compound: duloxetine
    Inhibition of [3H]5-HT from human SERT expressed in HEK293 cells
    Inhibition of [3H]5-HT from human SERT expressed in HEK293 cells
    [PMID: 17267217]
    HEK293 IC50
    870 nM
    Compound: duloxetine
    Inhibition of [3H]DA from human DAT expressed in HEK293 cells
    Inhibition of [3H]DA from human DAT expressed in HEK293 cells
    [PMID: 17267217]
    HEK293 IC50
    6.6 nM
    Compound: 7
    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
    660 nM
    Compound: 7
    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
    8.9 nM
    Compound: 7
    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
    4 nM
    Compound: 2
    Inhibition of [3H]5-HT uptake at human 5HTT expressed in HEK293 cells
    Inhibition of [3H]5-HT uptake at human 5HTT expressed in HEK293 cells
    [PMID: 19359175]
    HEK293 IC50
    5 nM
    Compound: 2
    Inhibition of [3H]NA uptake at human NET expressed in HEK293 cells
    Inhibition of [3H]NA uptake at human NET expressed in HEK293 cells
    [PMID: 19359175]
    HEK293 IC50
    590 nM
    Compound: 2
    Inhibition of [3H]DA uptake at human DAT expressed in HEK293 cells
    Inhibition of [3H]DA uptake at human DAT expressed in HEK293 cells
    [PMID: 19359175]
    HEK293 IC50
    2.3 nM
    Compound: 5
    Displacement of [3H]citalopram from human SERT transfected in HEK293 cells after 3 hrs by Wallac counting analysis
    Displacement of [3H]citalopram from human SERT transfected in HEK293 cells after 3 hrs by Wallac counting analysis
    [PMID: 24900709]
    HEK293 IC50
    29 nM
    Compound: 5
    Displacement of [3H]Nisoxetine from human NET transfected in HEK293 cells after 3 hrs by Wallac counting analysis
    Displacement of [3H]Nisoxetine from human NET transfected in HEK293 cells after 3 hrs by Wallac counting analysis
    [PMID: 24900709]
    HEK293 IC50
    10.4 nM
    Compound: Duloxetine
    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
    515 nM
    Compound: Duloxetine
    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
    977 nM
    Compound: Duloxetine
    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
    10.4 nM
    Compound: duloxetine
    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]
    HEK293 IC50
    515 nM
    Compound: duloxetine
    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
    977 nM
    Compound: duloxetine
    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]
    JAR IC50
    3 nM
    Compound: 3
    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
    3 nM
    Compound: 5
    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
    3 nM
    Compound: 2
    Inhibition of human SERT expressed in human JAR cells
    Inhibition of human SERT expressed in human JAR cells
    [PMID: 20378347]
    MDCK IC50
    4 nM
    Compound: 3
    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

    Duloxetine ((S)-Duloxetine) inhibits the reuptake of serotonin and norepinephrine in the central nervous system. Duloxetine is also considered a less potent inhibitor of dopamine reuptake. However, duloxetine has no significant affinity for dopaminergic, adrenergic, cholinergic, histaminergic, opioid, glutamate, and GABA receptors and can therefore be considered to be a selective reuptake inhibitor at the 5-HT and NA transporters. Duloxetine undergoes extensive metabolism, but the major circulating metabolites do not contribute significantly to the pharmacologic activity. Major depressive disorder is believed to be due in part to an increase in pro-inflammatory cytokines within the central nervous system. Antidepressants including ones with a similar mechanism of action as duloxetine, i.e. serotonin metabolism inhibition, cause a decrease in proinflammatory cytokine activity and an increase in anti-inflammatory cytokines; this mechanism may apply to duloxetine in its effect on depression but research on cytokines specific to duloxetine therapy is lacking[1].
    The analgesic properties of duloxetine in the treatment of diabetic neuropathy and central pain syndromes such as fibromyalgia are believed to be due to sodium ion channel blockade[2].

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

    Clinical Trial
    Molecular Weight

    297.41

    Formula

    C18H19NOS

    CAS No.
    Appearance

    Oil

    Color

    Light brown to yellow

    SMILES

    CNCC[C@H](OC1=CC=CC2=C1C=CC=C2)C3=CC=CS3

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (336.24 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 3.3624 mL 16.8118 mL 33.6236 mL
    5 mM 0.6725 mL 3.3624 mL 6.7247 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Concentration
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    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    Concentration (final)

    C2

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    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: ≥ 5 mg/mL (16.81 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% Corn Oil

      Solubility: ≥ 5 mg/mL (16.81 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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.
    Purity & Documentation
    References

    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 (sealed storage, away from moisture). 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 3.3624 mL 16.8118 mL 33.6236 mL 84.0590 mL
    5 mM 0.6725 mL 3.3624 mL 6.7247 mL 16.8118 mL
    10 mM 0.3362 mL 1.6812 mL 3.3624 mL 8.4059 mL
    15 mM 0.2242 mL 1.1208 mL 2.2416 mL 5.6039 mL
    20 mM 0.1681 mL 0.8406 mL 1.6812 mL 4.2030 mL
    25 mM 0.1345 mL 0.6725 mL 1.3449 mL 3.3624 mL
    30 mM 0.1121 mL 0.5604 mL 1.1208 mL 2.8020 mL
    40 mM 0.0841 mL 0.4203 mL 0.8406 mL 2.1015 mL
    50 mM 0.0672 mL 0.3362 mL 0.6725 mL 1.6812 mL
    60 mM 0.0560 mL 0.2802 mL 0.5604 mL 1.4010 mL
    80 mM 0.0420 mL 0.2101 mL 0.4203 mL 1.0507 mL
    100 mM 0.0336 mL 0.1681 mL 0.3362 mL 0.8406 mL
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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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