Perhexiline

Cat. No.: HY-B1334: FAQs
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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

CAS No. : 6621-47-2

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Other In-stock Forms of Perhexiline:

Perhexiline maleate

Other Forms of Perhexiline:

Perhexiline maleate In-stock

2 Publications Citing Use of MCE Perhexiline

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Biological Activity
Purity & Documentation
References
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Description

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]
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
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

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.

6621-47-2

SMILES

C1(CC(C2CCCCC2)C3CCCCC3)NCCCC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

Perhexiline Related Classifications

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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:

Perhexiline6621-47-2Mitochondrial MetabolismApoptosisAnti-anginalcancerglioblastomaBBBmitochondrial dysfunctionHepG2CLL cellInhibitorinhibitorinhibit

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