Perhexiline
Based on 7 publication(s) in Google Scholar
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.
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- Pureté: 99.96%
- CAS No.: 6621-47-2
- Formule: C19H35N
- Masse moléculaire:277.49
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Chemical Information
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Solvant et solubilité
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Publications Citing Use of MedChemExpress (MCE) Perhexiline
More- Nat Genet. 2025 Mar;57(3):680-693. [Abstract]
- Acta Pharm Sin B. 2025 Jan;15(1):133-150. [Abstract]
- Adv Sci (Weinh). 2024 Apr 16:e2308945. [Abstract]
- EBioMedicine. 2026 Apr 27:127:106256. [Abstract]
- Cancer Metab. 2025 Mar 31;13(1):16. [Abstract]
- BMC Biol. 2024 Apr 12;22(1):83. [Abstract]
- Pestic Biochem Physiol. 2025 Dec 22;218:106908.
Customer Validation & Images
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WB
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Cell Proliferation/Viability Assay
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Histological Imaging/Staining
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Cell Imaging/Staining
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Bio/Physico-chemical Assay
Activité biologique
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CPT-1 |
CPT-2 |
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Cell Line
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Type | Value | Description | References |
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| HepG2 | IC50 |
11.3 μM
Compound: Perhexiline
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Cytotoxicity against human HepG2 cells assessed as growth inhibition by XTT assay
Cytotoxicity against human HepG2 cells assessed as growth inhibition by XTT assay
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[PMID: 36793433] |
| KB | IC50 |
14.8 μM
Compound: 44
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Cytotoxicity in human KB cells
Cytotoxicity in human KB cells
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[PMID: 21504156] |
| Vero | CC50 |
8.67 μM
Compound: Perhexiline
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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
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10.1101/2020.03.20.999730 |
| Vero | IC50 |
6.38 μM
Compound: Perhexiline
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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
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10.1101/2020.03.20.999730 |
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.
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Cell Line:HepG2 cells
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Concentration:5, 10, 15, 25 μM
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Incubation Time:2, 4, 6 h
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Result:Induced time- and concentration-dependent cytotoxicity in hepatic cells.
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Cell Line:HepG2 cells
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Concentration:5, 10, 15, 25 μM
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Incubation Time:2 h
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Result:Reduced Bcl-2 and Mcl-1 level, and increased Bad level.
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.
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Animal Model:Orthotopic glioblastoma mouse model[5]
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Dosage:80 mg/kg
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Administration:Oral gavage, for 3 days.
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Result:Reduces tumor size (MR imaging) and improves in overall survival.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 6621-47-2
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Appearance Solid
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Masse moléculaire 277.49
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Formule C19H35N
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Color White to off-white
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SMILES
C1(CC(C2CCCCC2)C3CCCCC3)NCCCC1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (7)
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Journal Impact Factor
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Most Recent
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Nat Genet
2025 Mar;57(3):680-693. PMID: 40069506
Perhexiline purchased from MedChemExpress. Usage Cited in: Nat Genet. 2025 Mar;57(3):680-693. [Abstract]
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. [Abstract]
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.
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Acta Pharm Sin B
GSFM: A genome-scale functional module transformation to represent drug efficacy for in silico drug discovery. [Abstract]2025 Jan;15(1):133-150. PMID: 40041913
Perhexiline purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Jan;15(1):133-150. [Abstract]
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. [Abstract]
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. [Abstract]
Reversal relationship between LUAD GSFM pattern and Perhexiline maleate GSFM pattern.
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Adv Sci (Weinh)
Loss of OVOL2 in Triple-Negative Breast Cancer Promotes Fatty Acid Oxidation Fueling Stemness Characteristics. [Abstract]2024 Apr 16:e2308945. PMID: 38627980 -
EBioMedicine
Integrated spatial multi-omics delineates fatty acid degradation fuels malignant evolution at the tumour periphery in cervical squamous cell carcinoma. [Abstract]2026 Apr 27:127:106256. PMID: 42048995 -
Cancer Metab
Unveiling the powerhouse: ASCL1-driven small cell lung cancer is characterized by higher numbers of mitochondria and enhanced oxidative phosphorylation. [Abstract]2025 Mar 31;13(1):16. PMID: 40165271 -
BMC Biol
Targeting of REST with rationally-designed small molecule compounds exhibits synergetic therapeutic potential in human glioblastoma cells. [Abstract]2024 Apr 12;22(1):83. PMID: 38609948 -
Solvant et solubilité
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. E. Marc Jolicoeur, et al. 27 - Refractory Angina. Chronic Coronary Artery Disease, 2018, 412-431.
[2]. Zhen Ren, et al. Mitochondrial dysfunction and apoptosis underlie the hepatotoxicity of perhexiline. Toxicol In Vitro. 2020 Dec;69:104987. [Content Brief]
[3]. P-P Liu, et al. Elimination of chronic lymphocytic leukemia cells in stromal microenvironment by targeting CPT with an antiangina drug perhexiline. Oncogene. 2016 Oct 27;35(43):5663-5673. [Content Brief]
[4]. Giovanni Licari, et al. Enantioselectivity in the tissue distribution of perhexiline contributes to different effects on hepatic histology and peripheral neural function in rats. Pharmacol Res Perspect. 2018 Jun;6(3):e00406. [Content Brief]
[5]. Shiva Kant, et al. Perhexiline Demonstrates FYN-mediated Antitumor Activity in Glioblastoma. Mol Cancer Ther. 2020 Jul;19(7):1415-1422. [Content Brief]
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 |
Perhexiline Related Classifications
HY-B1334 Related Classifications
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