1. Metabolic Enzyme/Protease Apoptosis
  2. 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.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Perhexiline maleate) that retains the same biological activity.

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

Perhexiline Chemical Structure

Perhexiline Chemical Structure

CAS No. : 6621-47-2

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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].

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.
SMILES

C1(CC(C2CCCCC2)C3CCCCC3)NCCCC1

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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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Perhexiline
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HY-B1334
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