2. GPCR/G Protein Neuronal Signaling Autophagy Metabolic Enzyme/Protease
  3. Dopamine Receptor Autophagy Cytochrome P450 5-HT Receptor
  4. Chlorpromazine hydrochloride

Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis.

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Chlorpromazine hydrochloride Chemical Structure

Chlorpromazine hydrochloride Chemical Structure

CAS No. : 69-09-0

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Based on 55 publication(s) in Google Scholar

Other Forms of Chlorpromazine hydrochloride:

Chlorpromazine hydrochloride Related Antibodies

Top Publications Citing Use of Products

54 Publications Citing Use of MCE Chlorpromazine hydrochloride

IF

    Chlorpromazine hydrochloride purchased from MedChemExpress. Usage Cited in: Commun Biol. 2022 Nov 14;5(1):1248.  [Abstract]

    Chlorpromazine (CPZ) (10 µM; 30 min) remarkably decreases the cellular internalization of FITC-P-LPK in HCT116 cells. Chlorpromazine can inhibit clathrin-mediated endocytosis. The fluorescence intensity is observed by confocal microscopy and detected using a multi-well plate reader.

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    Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

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    CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

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    5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis[1][2][3][4][5].

    IC50 & Target

    D2 dopamine receptors; 5-HT2A[1][6].
    In Vitro

    Chlorpromazine hydrochloride (0, 10, 20, 40 μM; 0, 24, 48 h) inhibits growth of U-87MG glioma cells in a dose- and time- dependent manner[2].
    Chlorpromazine hydrochloride (20 μM; 0, 12, 24, 48 h) decreases the levels of cyclin A and cyclin B1 in U-87MG glioma cells, 12 h later[2].
    Chlorpromazine hydrochloride (20 μM) causes inhibition of cell cycle progression[2].
    Chlorpromazine hydrochloride (10 μM; 1 h) significantly suppresses the sEV internalization and dramatically reduces MDSCs in sEV-treated bone marrow cells (MDSCs can significantly suppress the immune cell response, causing immunosuppression in cancer cells)[3].
    Chlorpromazine hydrochloride (3, 10, 20, 40, 60 μM) blocks the hNav1.7 current in a concentration-dependent manner[4].
    Chlorpromazine hydrochloride blocks HERG potassium channels with an IC50 value of 21.6 μM and a Hill coefficient of 1.11[5].

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

    Chlorpromazine hydrochloride Related Antibodies

    Cell Proliferation Assay[2]

    Cell Line: U-87MG glioma cells
    Concentration: 0, 10, 20, 40 μM
    Incubation Time: 0, 24, 48 h
    Result: Showed anti-proliferative activity in a dose- and time-dependent manner.

    Immunofluorescence[3]

    Cell Line: Bone marrow cells (sEV-treated)
    Concentration: 10 µM
    Incubation Time: 1 h
    Result: Reduced MDSCs and suppressed the sEV internalization.

    Western Blot Analysis[2]

    Cell Line: U-87MG glioma cells
    Concentration: 20 μM
    Incubation Time: 0, 12, 24, 48 h
    Result: Decreased the levels of cyclin A and cyclin B1 12 h later, whereas levels of cyclin D1, proliferating cell nuclear antigen and GAPDH remained unchanged.
    In Vivo

    Chlorpromazine hydrochloride (20 mg/kg; i.p.; single daily for 7 days) inhibits xenograft tumor growth in nude mouse[2].

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

    Animal Model: 5- to 6-week-old athymic nude mice bearing intracranial U-87MG xenograft tumors[2].
    Dosage: 20 mg/kg
    Administration: Injected intraperitoneally; single daily for 7 days
    Result: Inhibited tumor growth on day 17.
    Molecular Weight

    355.33

    Formula

    C17H20Cl2N2S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CN(C)CCCN1C2=C(C=CC=C2)SC3=CC=C(Cl)C=C13.Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture and light

    *The compound is unstable in solutions, freshly prepared is recommended.

    Solvent & Solubility
    In Vitro: 

    H2O : 100 mg/mL (281.43 mM; Need ultrasonic)

    DMSO : ≥ 60 mg/mL (168.86 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.8143 mL 14.0714 mL 28.1429 mL
    5 mM 0.5629 mL 2.8143 mL 5.6286 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    * 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

    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:

    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: ≥ 200 mg/mL (562.86 mM); Clear solution

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

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    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: 99.90%

    COA (250 KB) HNMR (146 KB) LCMS (104 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 2.8143 mL 14.0714 mL 28.1429 mL 70.3571 mL
    5 mM 0.5629 mL 2.8143 mL 5.6286 mL 14.0714 mL
    10 mM 0.2814 mL 1.4071 mL 2.8143 mL 7.0357 mL
    15 mM 0.1876 mL 0.9381 mL 1.8762 mL 4.6905 mL
    20 mM 0.1407 mL 0.7036 mL 1.4071 mL 3.5179 mL
    25 mM 0.1126 mL 0.5629 mL 1.1257 mL 2.8143 mL
    30 mM 0.0938 mL 0.4690 mL 0.9381 mL 2.3452 mL
    40 mM 0.0704 mL 0.3518 mL 0.7036 mL 1.7589 mL
    50 mM 0.0563 mL 0.2814 mL 0.5629 mL 1.4071 mL
    60 mM 0.0469 mL 0.2345 mL 0.4690 mL 1.1726 mL
    80 mM 0.0352 mL 0.1759 mL 0.3518 mL 0.8795 mL
    100 mM 0.0281 mL 0.1407 mL 0.2814 mL 0.7036 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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    Chlorpromazine hydrochloride Related Classifications

    Help & FAQs
    • 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.

    Keywords:

    Chlorpromazine69-09-0Dopamine ReceptorAutophagyCytochrome P4505-HT ReceptorCYPsSerotonin Receptor5-hydroxytryptamine ReceptoraLQTSU-87MG glioma cellsBone marrow cellscancerschizophreniaCcOtumour immune escapeanalgesiccardiac arrhythmicInhibitorinhibitorinhibit

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