Perhexiline 是一种具有口服活性的CPT1和CPT2抑制剂，可减少脂肪酸代谢。Perhexiline 在肝细胞中诱导线粒体功能障碍和细胞凋亡 (apoptosis)。Perhexiline 可穿过血脑屏障 (BBB)，并显示出抗肿瘤活性。Perhexiline 可用于癌症和心绞痛等心血管疾病的研究。
| 生物活性 | Perhexiline is an orally activeCPT1andCPT2inhibitor that reduces fatty acid metabolism. Perhexiline induces mitochondrial dysfunction andapoptosisin hepatic cells. Perhexiline can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline can be used in the research of cancers, andcardiovascular diseaselike angina[1][2][5]. |
体外研究
(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].
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. |
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体内研究
(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].
| 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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