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

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

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Imipramine hydrochloride Chemical Structure

Imipramine hydrochloride Chemical Structure

CAS No. : 113-52-0

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Based on 4 publication(s) in Google Scholar

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Description

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

IC50 & Target

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

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: SW-480, DLD-1, and HCT-116
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.

Cell Autophagy Assay[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.
Clinical Trial
Molecular Weight

316.87

Formula

C19H25ClN2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN(C)CCCN1C2=CC=CC=C2CCC3=CC=CC=C31.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (315.59 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 62.5 mg/mL (197.24 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1559 mL 15.7793 mL 31.5587 mL
5 mM 0.6312 mL 3.1559 mL 6.3117 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, 1 years; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Dilution Calculator

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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: ≥ 2.5 mg/mL (7.89 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 (7.89 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 60 mg/mL (189.35 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.93%

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, 1 years; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.1559 mL 15.7793 mL 31.5587 mL 78.8967 mL
5 mM 0.6312 mL 3.1559 mL 6.3117 mL 15.7793 mL
10 mM 0.3156 mL 1.5779 mL 3.1559 mL 7.8897 mL
15 mM 0.2104 mL 1.0520 mL 2.1039 mL 5.2598 mL
20 mM 0.1578 mL 0.7890 mL 1.5779 mL 3.9448 mL
25 mM 0.1262 mL 0.6312 mL 1.2623 mL 3.1559 mL
30 mM 0.1052 mL 0.5260 mL 1.0520 mL 2.6299 mL
40 mM 0.0789 mL 0.3945 mL 0.7890 mL 1.9724 mL
50 mM 0.0631 mL 0.3156 mL 0.6312 mL 1.5779 mL
60 mM 0.0526 mL 0.2630 mL 0.5260 mL 1.3149 mL
80 mM 0.0394 mL 0.1972 mL 0.3945 mL 0.9862 mL
100 mM 0.0316 mL 0.1578 mL 0.3156 mL 0.7890 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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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