1. Neuronal Signaling Autophagy Apoptosis
  2. Serotonin Transporter Autophagy Apoptosis
  3. Imipramine

Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects.

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CAS No. : 50-49-7

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Imipramine:

Top Publications Citing Use of Products

    Imipramine purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Jan 6:147:113969.  [Abstract]

    Cells were exposed to moclobemide, milnacipran, venlafaxine, escitalopram, amitriptyline, trazodone, fluvoxamine, or Imipramine (0–100 μM concentration) for 24 h. Cell viability was assessed with CCK-8 assays.

    Imipramine purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Jan 6:147:113969.  [Abstract]

    CCK-8 assays for 24 h, 48 h and 72 h in KYSE30 and KYSE150 cells treated with various concentrations of Imipramine.

    Imipramine purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Jan 6:147:113969.  [Abstract]

    Colony formation assays in KYSE30 and KYSE150 cells treated with Imipramine (0, 50, or 100 μM, 14 days) . Histograms represent the number of colonies per set of replicates, according to colony formation measurements (n = 3).

    Imipramine purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Jan 6:147:113969.  [Abstract]

    Imipramine (0, 50, or 100 μM, 48 h). KYSE30 and KYSE150 cells showing migration or invasion in Transwell assays were fixed and stained. Cells that crossed the membranes were counted under a light microscope (10 × ) in three random fields of view.

    Imipramine purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Jan 6:147:113969.  [Abstract]

    Imipramine (0, 50, or 100 μM, 48 h) induces apoptosis in ESCC cells. ESCC or HET-1A cells were treated with various concentrations of Imipramine for 48 h. Cell apoptosis was detected by flow cytometry with annexin V-FITC/Caspase-3 double staining.

    Imipramine purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Jan 6:147:113969.  [Abstract]

    ESCC cells were treated with various concentrations of Imipramine (50, 100 μM) for 48 h. Western blotting was performed to assess Bax, Bcl-2, and cleaved-caspase-3 expression.

    Imipramine purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Jan 6:147:113969.  [Abstract]

    Anti-tumor effect of Imipramine (receiving intraperitoneal injections of 20 mg/kg/day, 15 days) in a xenograft model.Representative images depicting the appearance of tumors at the conclusion of treatment. Tumor volumes were measured every 3 days. Final tumor weights.

    Imipramine purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Jan 6:147:113969.  [Abstract]

    Imipramine (receiving intraperitoneal injections of 20 mg/kg/day, 15 days). Expression of P62, ATG5-ATG12 complex, Bcl-2, Bax, and Ki-67 was detected by IHC staining in tumor tissues.

    Imipramine purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2023 May 25;21(1):123.  [Abstract]

    LPS-primed BMDMs were stimulated with Imipramine (40 μM, 12 h). Western blot assessed the expression of caspase-1 and IL-1β in SN and GSDMD cleavage in WCL.

    Imipramine purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2023 May 25;21(1):123.  [Abstract]

    BMDMs were incubated with LPS and MCC950 and then treated with Imipramine (40 μM, 12 h). The expressions of IL-1β and caspase-1 in SN as well as GSDMD cleavage in WCL were evaluated using western blotting.
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    Description

    Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects[1][2][3][4][5].

    IC50 & Target

    Fascin1, Serotonin Transporter, Autophagy, Apoptosis[1][2][3][5]
    IC50: 32 nM (human placental serotonin transporter)[5]

    Cellular Effect
    Cell Line Type Value Description References
    CHO IC50
    5.1 nM
    Compound: Imipramine
    Inhibition of human SERT expressed in CHO cell membranes assessed as reduction in [3H]serotonin uptake preincubated for 10 mins followed by [3H]serotonin addition measured after 20 mins by liquid scintillation counting method
    Inhibition of human SERT expressed in CHO cell membranes assessed as reduction in [3H]serotonin uptake preincubated for 10 mins followed by [3H]serotonin addition measured after 20 mins by liquid scintillation counting method
    [PMID: 27865645]
    CHO IC50
    8.8 x 10-10 M
    Compound: Imipramine
    Displacement of [3H]imipramine from human recombinant 5-HT transporter expressed in CHO cells
    Displacement of [3H]imipramine from human recombinant 5-HT transporter expressed in CHO cells
    [PMID: 26988801]
    CHO IC50
    8.8 x 10-10 M
    Compound: Imipramine
    Displacement of [3H]imipramine from human recombinant 5HT transporter expressed in CHO cells measured after 60 mins by scintillation counting method
    Displacement of [3H]imipramine from human recombinant 5HT transporter expressed in CHO cells measured after 60 mins by scintillation counting method
    [PMID: 27876250]
    DG-75 IC50
    > 50 μM
    Compound: Imipramine
    Reduction in cell viability of human DG75 cells after 24 hrs by Alamar blue viability assay
    Reduction in cell viability of human DG75 cells after 24 hrs by Alamar blue viability assay
    [PMID: 23385211]
    HEK293 IC50
    0.008 μM
    Compound: Imipramine
    Inhibition of [3H]5HT uptake at human SERT expressed in HEK293 cells
    Inhibition of [3H]5HT uptake at human SERT expressed in HEK293 cells
    [PMID: 17846138]
    HEK293 IC50
    0.074 μM
    Compound: Imipramine
    Inhibition of [3H]norepinephrine uptake at human NET expressed in HEK293 cells
    Inhibition of [3H]norepinephrine uptake at human NET expressed in HEK293 cells
    [PMID: 17846138]
    HEK293 IC50
    17.1 μM
    Compound: Imipramine
    Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
    Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
    [PMID: 18788725]
    HEK293 IC50
    2.6 nM
    Compound: 1
    Inhibition of human SERT W103A mutant expressed in HEK293 MSR cells assessed as [3H]-5-HT uptake preincubated for 30 mins followed addition of [3H]-5HT and compound for 10 mins by micro-scintillation counter
    Inhibition of human SERT W103A mutant expressed in HEK293 MSR cells assessed as [3H]-5-HT uptake preincubated for 30 mins followed addition of [3H]-5HT and compound for 10 mins by micro-scintillation counter
    [PMID: 27160055]
    HEK293 IC50
    25.6 μM
    Compound: Imipramine
    Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells
    Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells
    [PMID: 17846138]
    HEK293 IC50
    6.8 nM
    Compound: Imipramine
    Displacement of [3H]imipramin from human recombinant SERT over-expressed in HEK293 cells
    Displacement of [3H]imipramin from human recombinant SERT over-expressed in HEK293 cells
    [PMID: 24012181]
    HEK293 IC50
    7.95 μM
    Compound: Imipramine
    Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
    Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
    [PMID: 28230985]
    HeLa IC50
    40.74 μM
    Compound: Imipramine
    Reduction in cell viability of human HeLa cells after 24 hrs by Alamar blue viability assay
    Reduction in cell viability of human HeLa cells after 24 hrs by Alamar blue viability assay
    [PMID: 23385211]
    MDCK IC50
    16 μM
    Compound: Imipramine
    TP_TRANSPORTER: inhibition of TEA uptake (TEA: 50 uM) in OCT1-expressing MDCK cells
    TP_TRANSPORTER: inhibition of TEA uptake (TEA: 50 uM) in OCT1-expressing MDCK cells
    [PMID: 11758759]
    MDCK IC50
    9.9 μM
    Compound: Imipramine
    TP_TRANSPORTER: inhibition of TEA uptake (TEA: 50 uM) in OCT2-expressing MDCK cells
    TP_TRANSPORTER: inhibition of TEA uptake (TEA: 50 uM) in OCT2-expressing MDCK cells
    [PMID: 11758759]
    ScN2a EC50
    10 μM
    Compound: Imipramine
    Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells
    Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells
    [PMID: 12904059]
    ScN2a EC50
    5000 nM
    Compound: imipramine
    Inhibition of protease-resistant scrapie prion protein activity in ScN2a cells
    Inhibition of protease-resistant scrapie prion protein activity in ScN2a cells
    [PMID: 17064077]
    Ventricular myocyte IC50
    4.05 μM
    Compound: Imipramine
    Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
    Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
    [PMID: 22761000]
    Ventricular myocyte IC50
    8.3 μM
    Compound: Imipramine
    Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
    Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
    [PMID: 22761000]
    In Vitro

    Imipramine (0.5-300 μM, 3 days) inhibits HCT-116 cell viability[1].
    Imipramine (20 μM) inhibits cell migration (7 h) and invasion (48 h)[1].
    Imipramine (50 μM, 0-240 min) inhibites the PI3K/Akt/mTOR signaling pathway in U-87MG glioma cells[2].
    Imipramine (60 μM, 24 h) stimulates U-87MG glioma cells autophagy[2].
    Imipramine (80 μM, 24 h) induces HL-60 cell apoptosis[3].

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

    Cell Viability Assay[1]

    Cell Line: DLD-1, HCT-116, and SW-480
    Concentration: 0.5-300 μM
    Incubation Time: 3 days
    Result: Inhibited cell viability and HCT-116 was more sensitive than DLD-1 and SW-480.

    Cell Migration Assay [1]

    Cell Line: DLD-1, HCT-116, and SW-480
    Concentration: 20 μM
    Incubation Time: 7 h
    Result: Produced a remarkable inhibition of migration in all assayed cell lines.

    Cell Invasion Assay[1]

    Cell Line: HCT-116
    Concentration: 20 μM
    Incubation Time: 48 h
    Result: Inhibited cell invasion through Matrigel.

    Western Blot Analysis[2]

    Cell Line: U-87MG
    Concentration: 50 μM
    Incubation Time: 0, 15, 30, 60, 120 and 240 min
    Result: Markedly inhibited the phosphorylation of both Akt (Ser473) and mTOR (Ser2481) in a time-dependent manner. Also dephosphorylated p70 S6K, a downstream target of mTOR.

    Cell Autophagy Assay[2]

    Cell Line: U-87MG
    Concentration: 60 μM
    Incubation Time: 24 h
    Result: Stimulated the induction of autophagy through the redistribution of LC3 in U-87MG glioma cells.

    Apoptosis Analysis[3]

    Cell Line: HL-60
    Concentration: 80 μM
    Incubation Time: 24 h
    Result: Induced cell apoptosis.
    In Vivo

    Imipramine (20 mg/kg, i.p. or 15 mg/kg, p.o.; daily for 24 days) attenuates neuroinflammatory signaling and reverses stress-induced social avoidance in mice[4].

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

    Animal Model: Male C57BL/6 mice (6–8 weeks old) subjected to RSD (repeated social defeat) and HCC (home cage control)[4]
    Dosage: 20 mg/kg or 15 mg/kg
    Administration: Intraperitoneal injection or oral administration, daily for 24 days
    Result: Reversed RSD-induced social avoidance behavior, significantly increasing the interaction time, significantly decreased stress-induced mRNA levels for IL-6 in brain microglia.
    Molecular Weight

    280.41

    Formula

    C19H24N2

    CAS No.
    Appearance

    Viscous Liquid

    Color

    Colorless to light yellow

    SMILES

    CN(C)CCCN1C2=CC=CC=C2CCC3=CC=CC=C31

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Pure form -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 200 mg/mL (713.24 mM; ultrasonic and warming and heat to 60°C; 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 3.5662 mL 17.8310 mL 35.6621 mL
    5 mM 0.7132 mL 3.5662 mL 7.1324 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.

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    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 (17.83 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 5 mg/mL (17.83 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 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
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    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).
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    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.
    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. 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 3.5662 mL 17.8310 mL 35.6621 mL 89.1552 mL
    5 mM 0.7132 mL 3.5662 mL 7.1324 mL 17.8310 mL
    10 mM 0.3566 mL 1.7831 mL 3.5662 mL 8.9155 mL
    15 mM 0.2377 mL 1.1887 mL 2.3775 mL 5.9437 mL
    20 mM 0.1783 mL 0.8916 mL 1.7831 mL 4.4578 mL
    25 mM 0.1426 mL 0.7132 mL 1.4265 mL 3.5662 mL
    30 mM 0.1189 mL 0.5944 mL 1.1887 mL 2.9718 mL
    40 mM 0.0892 mL 0.4458 mL 0.8916 mL 2.2289 mL
    50 mM 0.0713 mL 0.3566 mL 0.7132 mL 1.7831 mL
    60 mM 0.0594 mL 0.2972 mL 0.5944 mL 1.4859 mL
    80 mM 0.0446 mL 0.2229 mL 0.4458 mL 1.1144 mL
    100 mM 0.0357 mL 0.1783 mL 0.3566 mL 0.8916 mL
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