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

Perhexiline is an orally active CPT1 and CPT2 inhibitor that reduces fatty acid metabolism. Perhexiline induces mitochondrial dysfunction and apoptosis in hepatic cells. Perhexiline can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline 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. : 6621-47-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Perhexiline:

Top Publications Citing Use of Products

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

    IC50 & Target

    CPT-1

     

    CPT-2

     

    Cellular Effect
    Cell Line Type Value Description References
    HepG2 IC50
    11.3 μM
    Compound: Perhexiline
    Cytotoxicity against human HepG2 cells assessed as growth inhibition by XTT assay
    Cytotoxicity against human HepG2 cells assessed as growth inhibition by XTT assay
    [PMID: 36793433]
    KB IC50
    14.8 μM
    Compound: 44
    Cytotoxicity in human KB cells
    Cytotoxicity in human KB cells
    [PMID: 21504156]
    Vero CC50
    8.67 μM
    Compound: Perhexiline
    Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
    Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
    10.1101/2020.03.20.999730
    Vero IC50
    6.38 μM
    Compound: Perhexiline
    Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
    Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
    10.1101/2020.03.20.999730
    In Vitro

    Perhexiline (5-25 μM, 2-6 h) reduces cell viability in HepG2 cells[2].
    Perhexiline (5-25 μM, 2-6 h) reduces cellular ATP content and Lactate dehydrogenase (LDH) release in HepG2 cells[2].
    Perhexiline (20 μM, 2 h) activates caspase 3/7 in HepG2 cells[2].
    Perhexiline (5-25 μM, 4 h) causes mitochondrial dysfunction in HepG2 cells[2].
    Perhexiline (5 μM, 48 h) 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) reduces peripheral neural function in female DA rats[4].
    Perhexiline (80 mg/kg, oral gavage, for 3 days) 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.
    Clinical Trial
    Molecular Weight

    277.49

    Formula

    C19H35N

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    C1(CC(C2CCCCC2)C3CCCCC3)NCCCC1

    Shipping

    Room temperature in continental US; may vary elsewhere.

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

    DMSO : ≥ 100 mg/mL (360.37 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 3.6037 mL 18.0187 mL 36.0373 mL
    5 mM 0.7207 mL 3.6037 mL 7.2075 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.

    • 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)

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    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
    Purity & Documentation

    Purity: 99.96%

    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 3.6037 mL 18.0187 mL 36.0373 mL 90.0933 mL
    5 mM 0.7207 mL 3.6037 mL 7.2075 mL 18.0187 mL
    10 mM 0.3604 mL 1.8019 mL 3.6037 mL 9.0093 mL
    15 mM 0.2402 mL 1.2012 mL 2.4025 mL 6.0062 mL
    20 mM 0.1802 mL 0.9009 mL 1.8019 mL 4.5047 mL
    25 mM 0.1441 mL 0.7207 mL 1.4415 mL 3.6037 mL
    30 mM 0.1201 mL 0.6006 mL 1.2012 mL 3.0031 mL
    40 mM 0.0901 mL 0.4505 mL 0.9009 mL 2.2523 mL
    50 mM 0.0721 mL 0.3604 mL 0.7207 mL 1.8019 mL
    60 mM 0.0601 mL 0.3003 mL 0.6006 mL 1.5016 mL
    80 mM 0.0450 mL 0.2252 mL 0.4505 mL 1.1262 mL
    100 mM 0.0360 mL 0.1802 mL 0.3604 mL 0.9009 mL
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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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    Product Name:
    Perhexiline
    Cat. No.:
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