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[2].IC50 & Target:IC50: 77 μM (Rat heart CPT 1), 148 μM (Rat liver CPT 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).
In Vivo:Perhexiline (200 mg/kg, p.o., daily for 8 weeks) maleate reduces peripheral neural function in female DA rats.
Perhexiline (80 mg/kg, oral gavage, for 3 days) maleate demonstrates anti-tumor activity in glioblastoma mouse model.