1. GPCR/G Protein Neuronal Signaling Stem Cell/Wnt MAPK/ERK Pathway NF-κB Immunology/Inflammation Apoptosis Metabolic Enzyme/Protease
  2. Adrenergic Receptor ERK JNK p38 MAPK NF-κB AP-1 Apoptosis Reactive Oxygen Species (ROS) Mitochondrial Metabolism TNF Receptor
  3. Desipramine hydrochloride

Desipramine hydrochloride is a first-generation tricyclic antidepressant. Desipramine hydrochloride selectively binds to norepinephrine transporter and blocks neuronal norepinephrine reuptake. Desipramine hydrochloride activates MAPK signaling via ERK1/2, JNK, and p38, represses NF-κB and AP-1 activity, and induces apoptosis via ROS elevation, mitochondrial membrane potential reduction, and intracellular calcium increase. Desipramine hydrochloride also shows anyi-inflammatory activity, inhibiting TNF-α production. Desipramine hydrochloride can be used for the research of hepatocellular cancer, inflammation, and neurological diseases.

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

CAS No. : 58-28-6

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Customer Review

Based on 15 publication(s) in Google Scholar

Other Forms of Desipramine hydrochloride:

Top Publications Citing Use of Products

    Desipramine hydrochloride purchased from MedChemExpress. Usage Cited in: Sci Total Environ. 2024 May 1:923:171405.  [Abstract]

    Desipramine hydrochloride (Des; 0-50 μM; 24 h). Cell viability of BRL-3A cells after Des intervention was detected by CCK-8. Other groups were compared with 0 μM group.

    Desipramine hydrochloride purchased from MedChemExpress. Usage Cited in: Sci Total Environ. 2024 May 1:923:171405.  [Abstract]

    Desipramine hydrochloride (Des; 12.5 μM; 24 h). The expression levels of apoptosis-related proteins in BRL-3A cells were detected by western blotting.

    Desipramine hydrochloride purchased from MedChemExpress. Usage Cited in: Sci Total Environ. 2024 May 1:923:171405.  [Abstract]

    Desipramine hydrochloride (Des; 12.5 μM; 24 h). Hoechst/PI double staining: Hoechst/PI was used to double stain and observe them under fluorescence microscope (200×). Hoechst 33342 can stain the nucleus with blue fluorescence. PI can stain necrotic cells with red fluorescence.

    Desipramine hydrochloride purchased from MedChemExpress. Usage Cited in: Sci Total Environ. 2024 May 1:923:171405.  [Abstract]

    Desipramine hydrochloride (Des; 12.5 μM; 24 h). The level of LDH in cell culture medium after 12.5 μM Des intervention and/or 20 μM Cadmium exposure for 24 h.

    Desipramine hydrochloride purchased from MedChemExpress. Usage Cited in: Pharmaceutics. 2022 Jul 22;14(8):1523.

    Figure shows that 10 and 30 μM of Desipramine hydrochloride attenuated EGCG-induced enhancement of MNPcell by 8.9% and 39.3% in the Mag− group, respectively. In the Mag+ group, MNPcell was enhanced up to 6.6-fold by EGCG compared with the control group, which was minorly attenuated by 5.7% and 11.2% by Desipramine hydrochloride at 10 and 30 μM, respectively.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Desipramine hydrochloride is a first-generation tricyclic antidepressant. Desipramine hydrochloride selectively binds to norepinephrine transporter and blocks neuronal norepinephrine reuptake. Desipramine hydrochloride activates MAPK signaling via ERK1/2, JNK, and p38, represses NF-κB and AP-1 activity, and induces apoptosis via ROS elevation, mitochondrial membrane potential reduction, and intracellular calcium increase. Desipramine hydrochloride also shows anyi-inflammatory activity, inhibiting TNF-α production. Desipramine hydrochloride can be used for the research of hepatocellular cancer, inflammation, and neurological diseases[1][2][3][4].

    IC50 & Target[1]

    ERK1

     

    ERK2

     

    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    0.0063 μM
    Compound: Desipramine
    Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells (PubChem AID: 1745860)
    Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells (PubChem AID: 1745860)
    [PMID: 34112854]
    In Vitro

    Desipramine hydrochloride (3-500 µM; 24 h) reduces the viability of human hepatoma Hep3B cells in a dose-dependent manner[1].
    Desipramine hydrochloride (10-500 µM; 24 h) induces cytotoxicity in human hepatoma Hep3B cells in a dose-dependent manner, as measured by increased LDH release[1].
    Desipramine hydrochloride (3-100 µM; 24 h) increases intracellular ROS production in human hepatoma Hep3B cells in a dose-dependent manner[1].
    Desipramine hydrochloride (3-100 µM µM; 24 h) has its induced cell death in human hepatoma Hep3B cells abolished by the ROS scavenger NAC (HY-B0215) at concentrations up to 30 µM, and partially reduced at 100 µM after 24 h[1].
    Desipramine hydrochloride (3-100 µM; 24 h) reduces mitochondrial membrane potential in human hepatoma Hep3B cells in vitro in a dose-dependent manner[1].
    Desipramine hydrochloride (100 µM; 1-8 h) activates ERK1/2, JNK, and p38 MAPK signaling in human hepatoma Hep3B cells-[1].
    Desipramine hydrochloride (3-100 µM; 24 h) has its induced cell death in human hepatoma Hep3B cells abolished by inhibition of ERK1/2, p38, or JNK MAPK signaling[1].
    Desipramine hydrochloride (30-500 µM) increases intracellular calcium levels in human hepatoma Hep3B cells in a concentration-dependent manner, with increases occurring via both extracellular calcium influx and intracellular calcium release[1].
    Desipramine hydrochloride potently binds to the rat norepinephrine transporter with a Ki of 6.2 nM, showing 25-fold selectivity over the rat serotonin transporter (Ki = 158 nM) [3].
    Desipramine hydrochloride (1 h) binds to the rat α2D-adrenoceptor with a Ki of 3.4 μM[3].
    Desipramine hydrochloride potently binds to the human norepinephrine transporter with a Ki of 0.63 nM, has lower affinity for the human serotonin transporter (Ki = 22 nM), and lacks affinity for the human dopamine transporter (Ki >10,000 nM)[3].
    Desipramine hydrochloride (0.01-10 μM; 20 h) dose-dependently inhibits LPS (HY-D1056)-induced TNF-α release from primary human monocytes[4].
    Desipramine hydrochloride (10 μM) reduces TNF-α-induced RANTES release and RANTES mRNA accumulation in A549 human lung epithelial cells[4].
    Desipramine hydrochloride (10 μM) represses TNF-α-induced NF-κB activity in A549 human lung epithelial cells[4].
    Desipramine hydrochloride (10 μM) reduces TPA (HY-18739)-induced AP-1 activity in A549 human lung epithelial cells[4].

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

    Cell Viability Assay[1]

    Cell Line: human hepatoma Hep3B cells
    Concentration: 1 µM, 3 µM, 10 µM, 30 µM, 100 µM, 300 µM, 500 µM
    Incubation Time: 24 h
    Result: Did not affect cell viability at 1 µM.
    Reduced cell viability to 90.2% of control at 3 µM.
    Reduced cell viability to 87.4% of control at 10 µM.
    Reduced cell viability to 69.1% of control at 30 µM.
    Reduced cell viability to 45.9% of control at 100 µM.
    Reduced cell viability to 36.1% of control at 300 µM.
    Reduced cell viability to 27.8% of control at 500 µM.
    Caused statistically significant viability reductions at concentrations ≥3 µM compared to control.

    Western Blot Analysis[1]

    Cell Line: human hepatoma Hep3B cells
    Concentration: 100 µM
    Incubation Time: 1 h, 2 h, 4 h, 8 h
    Result: Increased phosphorylation of ERK1/2 to 185.2% of control at 1 h, 151.5% of control at 2 h, and 138.5% of control at 4 h.
    Increased phosphorylation of p38 to 135.1% of control at 1 h and 116.4% of control at 2 h.
    Increased phosphorylation of JNK to 118.9% of control at 1 h and 113.9% of control at 2 h.
    Maintained unchanged total levels of ERK1/2, JNK, and p38 across all time points.
    Caused statistically significant increases in MAPK phosphorylation at the specified time points compared to control.
    In Vivo

    Desipramine (5-20 mg/kg; i.p.; single dose, 30 minutes pre-LPS) hydrochloride dose-dependently inhibits LPS (HY-D1056)-induced serum TNF-α production and increases survival rate to 70% in a murine septic shock model[4].
    Desipramine (10 mg/kg; i.p.; daily; 8 days, 30 minutes pre-Ovalbumin nebulization) hydrochloride reduces lung inflammation by decreasing macrophage and lymphocyte counts in Ovalbumin (HY-W250978)-sensitized rats but does not attenuate bronchial hyperresponsiveness[4].

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

    Animal Model: LPS-induced BALB/c mice (5-week-old, 17-21 g)[4]
    Dosage: 5, 10, 20 mg/kg
    Administration: i.p.; single dose (preventive, 30 minutes pre-LPS)
    Result: Significantly inhibited LPS-induced serum TNF-α production.
    Increased mouse survival rate to 70% with preventive 20 mg/kg treatment (vs 10% in saline controls).
    Animal Model: Ovalbumin-sensitized Brown Norway rats (10-week-old)[4]
    Dosage: 10 mg/kg
    Administration: i.p.; daily; 8 days (30 minutes pre-ovalbumin nebulization)
    Result: Did not reduce bronchial hyperresponsiveness to metacholine (measured by enhanced pause, Penh).
    Reduced total number of inflammatory cells in bronchoalveolar lavages.
    Decreased macrophage count by 52% compared to saline-treated sensitized rats.
    Decreased lymphocyte count by 21% compared to saline-treated sensitized rats.
    Did not reduce neutrophil or eosinophil counts compared to saline-treated sensitized rats.
    Clinical Trial
    Molecular Weight

    302.84

    Formula

    C18H23ClN2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CNCCCN1C2=CC=CC=C2CCC3=CC=CC=C31.Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

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

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (330.21 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 100 mg/mL (330.21 mM; Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.3021 mL 16.5104 mL 33.0207 mL
    5 mM 0.6604 mL 3.3021 mL 6.6041 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 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. 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.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

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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 (8.26 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 (8.26 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: 1 mg/mL (3.30 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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

    Dosage

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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: 99.76%

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

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 3.3021 mL 16.5104 mL 33.0207 mL 82.5518 mL
    5 mM 0.6604 mL 3.3021 mL 6.6041 mL 16.5104 mL
    10 mM 0.3302 mL 1.6510 mL 3.3021 mL 8.2552 mL
    15 mM 0.2201 mL 1.1007 mL 2.2014 mL 5.5035 mL
    20 mM 0.1651 mL 0.8255 mL 1.6510 mL 4.1276 mL
    25 mM 0.1321 mL 0.6604 mL 1.3208 mL 3.3021 mL
    30 mM 0.1101 mL 0.5503 mL 1.1007 mL 2.7517 mL
    40 mM 0.0826 mL 0.4128 mL 0.8255 mL 2.0638 mL
    50 mM 0.0660 mL 0.3302 mL 0.6604 mL 1.6510 mL
    60 mM 0.0550 mL 0.2752 mL 0.5503 mL 1.3759 mL
    80 mM 0.0413 mL 0.2064 mL 0.4128 mL 1.0319 mL
    100 mM 0.0330 mL 0.1651 mL 0.3302 mL 0.8255 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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