1. Metabolic Enzyme/Protease Apoptosis
  2. Carnitine Palmitoyltransferase (CPT) Mitochondrial Metabolism Apoptosis
  3. Perhexiline maleate

Perhexiline maleate is an orally active CPT1 and CPT2 inhibitor that reduces fatty acid metabolism. Perhexiline maleate induces mitochondrial dysfunction and apoptosis in hepatic cells. Perhexiline maleate can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline maleate can be used in the research of cancers, and cardiovascular disease like angina.

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

CAS No. : 6724-53-4

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Based on 6 publication(s) in Google Scholar

Other Forms of Perhexiline maleate:

Top Publications Citing Use of Products

    Perhexiline maleate purchased from MedChemExpress. Usage Cited in: Nat Genet. 2025 Mar;57(3):680-693.

    Inhibition of CPT1A activity using Perhexiline maleate (0-10 μM, 24 h) and PD-L1 detection by western blotting in A375 cell.

    Perhexiline maleate purchased from MedChemExpress. Usage Cited in: Nat Genet. 2025 Mar;57(3):680-693.

    A375 cells treated with Perhexiline maleate (0-10 μM) for 24 h, then co-cultured with or without activated T cells for 24 h to assess the killing effect.

    Perhexiline maleate purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Jan;15(1):133-150.

    Results of H&E and Ki67 staining in representative A549 cells tumor sections of vehicle, perhexiline (10 mg/kg, ip, 3 days), and Perhexiline maleate (10 mg/kg) treated naked mice. Scale bar = 200 μm (H&E up).

    Perhexiline maleate purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Jan;15(1):133-150.

    Perhexiline maleate (0-20 μM, 8 days) exhibited inhibition of colony formation in A549 and NCI-H1975 cells.

    Perhexiline maleate purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Jan;15(1):133-150.

    Reversal relationship between LUAD GSFM pattern and Perhexiline maleate GSFM pattern.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Perhexiline maleate is an orally active CPT1 and CPT2 inhibitor that reduces fatty acid metabolism. Perhexiline maleate induces mitochondrial dysfunction and apoptosis in hepatic cells. Perhexiline maleate can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline maleate can be used in the research of cancers, and cardiovascular disease like angina[1][2][5].

    IC50 & Target

    CPT-1

     

    CPT-2

     

    In Vitro

    Perhexiline (5-25 μM, 2-6 h) maleate reduces cell viability in HepG2 cells[2].
    Perhexiline (5-25 μM, 2-6 h) maleate reduces cellular ATP content and Lactate dehydrogenase (LDH) release in HepG2 cells[2].
    Perhexiline (20 μM, 2 h) maleate activates caspase 3/7 in HepG2 cells[2].
    Perhexiline (5-25 μM, 4 h) maleate causes mitochondrial dysfunction in HepG2 cells[2].
    Perhexiline (5 μM, 48 h) maleate selectively induces massive apoptosis in CLL cells (high expression of CPT)[3].

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

    Cell Viability Assay[2]

    Cell Line: HepG2 cells
    Concentration: 5, 10, 15, 25 μM
    Incubation Time: 2, 4, 6 h
    Result: Induced time- and concentration-dependent cytotoxicity in hepatic cells.

    Western Blot Analysis[2]

    Cell Line: HepG2 cells
    Concentration: 5, 10, 15, 25 μM
    Incubation Time: 2 h
    Result: Reduced Bcl-2 and Mcl-1 level, and increased Bad level.
    In Vivo

    Perhexiline (200 mg/kg, p.o., daily for 8 weeks) maleate reduces peripheral neural function in female DA rats[4].
    Perhexiline (80 mg/kg, oral gavage, for 3 days) maleate demonstrates anti-tumor activity in glioblastoma mouse model[5].

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

    Animal Model: Orthotopic glioblastoma mouse model[5]
    Dosage: 80 mg/kg
    Administration: Oral gavage, for 3 days.
    Result: Reduces tumor size (MR imaging) and improves in overall survival.
    Molecular Weight

    393.56

    Formula

    C23H39NO4

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O)/C=C\C(O)=O.C1(CC(C2CCCCC2)C3CCCCC3)NCCCC1

    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 : 16.67 mg/mL (42.36 mM; ultrasonic and adjust pH to 5 with HCl; 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 2.5409 mL 12.7045 mL 25.4091 mL
    5 mM 0.5082 mL 2.5409 mL 5.0818 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Concentration (final)

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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:  0.5% CMC-Na/saline water

      Solubility: 5 mg/mL (12.70 mM); Suspended solution; Need ultrasonic

    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.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.97%

    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 2.5409 mL 12.7045 mL 25.4091 mL 63.5227 mL
    5 mM 0.5082 mL 2.5409 mL 5.0818 mL 12.7045 mL
    10 mM 0.2541 mL 1.2705 mL 2.5409 mL 6.3523 mL
    15 mM 0.1694 mL 0.8470 mL 1.6939 mL 4.2348 mL
    20 mM 0.1270 mL 0.6352 mL 1.2705 mL 3.1761 mL
    25 mM 0.1016 mL 0.5082 mL 1.0164 mL 2.5409 mL
    30 mM 0.0847 mL 0.4235 mL 0.8470 mL 2.1174 mL
    40 mM 0.0635 mL 0.3176 mL 0.6352 mL 1.5881 mL
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    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.

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    Product Name:
    Perhexiline maleate
    Cat. No.:
    HY-B1334A
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