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MedChemExpress - Model Perhexiline maleate - 6724-53-4

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].

Perhexiline maleate

MCE China：Perhexiline maleate

Brand：MedChemExpress (MCE)

Cat. No.HY-B1334A

CAS：6724-53-4

Purity：99.26%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

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.

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].

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].

IC50 & Target：IC50: 77 μM (Rat heart CPT 1), 148 μM (Rat liver CPT 1)[1] 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. 0 --> Perhexiline maleate Related Antibodies Cell Viability Assay[2] Cell Line: HepG2 cells

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]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
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•   The biological activity of the products has been verified by the experiments of customers in various countries；
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