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Perhexiline (maleate) Sale

(Synonyms: 马来酸哌克昔林) 目录号 : GC15257

Inhibitor of carnitine palmitoyltransferases

Perhexiline (maleate) Chemical Structure

Cas No.:6724-53-4

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1mg
¥477.00
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10mg
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment:

The effect of antitumoral drugs on neuroblastoma cell survival is evaluated using the MTT assay. Approximately 24 hours after plating, cells are exposed to Perhexiline maleate (0.01 μM) for 48 hours at 37°C. Cytotoxicity is expressed as the percentage of cells surviving in relation to untreated cells[2].

Animal experiment:

Mice: In protocol a, 21 mice are divided in 4 groups: control vehicle group: DMSO; cisplatin (3 mg/kg/dose) treated group; Perhexiline (1 mg/kg/dose) treated group and; Perhexiline (1 mg/kg/dose) and cisplatin (3 mg/kg/dose) treated group. In protocol b, 20 mice are divided in 4 groups: control vehicle group: DMSO; Perhexiline (3 mg/kg/dose) treated group; cisplatin (5 mg/kg/dose) treated group; Perhexiline (3 mg/kg/dose) and cisplatin (5 mg/kg/dose) treated group[2].

References:

[1]. Kennedy JA, et al. Inhibition of carnitine palmitoyltransferase-1 in rat heart and liver by Perhexiline and amiodarone. Biochem Pharmacol. 1996 Jul 26;52(2):273-80.
[2]. Vella S, et al. Perhexiline maleate enhances antitumor efficacy of cisplatin in neuroblastoma by inducing over-expression of NDM29 ncRNA. Sci Rep. 2015 Dec 17;5:18144.

产品描述

Perhexiline maleate, an anti-anginal metabolic modulator, blocks the mitochondrial enzyme carnitine palmitoyltransferase 1 (CPT1) and to a lesser extent CPT2, which triggers causes a shift in myocardial substrate utilization from long chain fatty acids to carbohydrates, leading to the increased glucose and lactate utilization and increased ATP production for the same O2 consumption and consequently improves myocardial efficiency.

CPT1 and CPT2 are mitochondrial enzymes which oxidize long-chain fatty acids in the mitochondria. Additionally, perhexiline maleate is found to suppress the activity of Mammalian target of rapamycin complex 1 (mTORC1) which controls the initiation step of protein synthesis via the phosphorylation of eukaryotic initiation factor 4E-binding proteins and of ribosomal S6 kinases.

In vitro: Perhexiline maleate concentration-dependently and competitively inhibited CPT1 in rat cardiac and hepatic mitochondria, with an IC50 value of 77 and 148 μM, respectively. It was indicated that perhexiline maleate displayed a greater sensitivity of the cardiac than the hepatic enzyme when exhibiting inhibition effect [1]. Perhexiline maleate produced concentration-dependent inhibition of CPT2 activity with an IC50 value of 79 μM [2]. In human breast cancer MCF-7 cells, Perhexiline maleate blocked mTORC1 signaling at 10 μM and elicited autophagy ~7-fold at a concentration of 10 μM [3].

In vivo: Adult mice of Swiss NMRI strain were orally administrated with perhexiline maleate at a dosage of 100 mg/kg body weight/day for 10 weeks. Perhexiline maleate triggered changes in nerve, including a few cytoplasmic inclusions in Schwann and perineurial cells of mice treated with perhexiline maleate. After 11 weeks of administration of the drug, and up to 18 weeks, small abnormal zones were displayed on several muscle fibers, which were formed by tubular aggregates [4].

References:
[1].  Kennedy, J., Unger, S., & Horowitz, J. Inhibition of carnitine palmitoyltransferase-1 in rat heart and liver by perhexiline and amiodarone. Biochemical Pharmacology. 1996; 52(2): 273-280.
[2].  Kennedy, J., Kiosoglous, A., Murphy, G., Pelle, M., & Horowitz, J. Effect of Perhexiline and Oxfenicine on Myocardial Function and Metabolism During Low-Flow Ischemia/Reperfusion in the Isolated Rat Heart. Journal of Cardiovascular Pharmacology. 2000; 36(6): 794-801.
[3].  Balgi, A., Fonseca, B., Donohue, E., Tsang, T., Lajoie, P., & Proud, C. et al. Screen for Chemical Modulators of Autophagy Reveals Novel Therapeutic Inhibitors of mTORC1 Signaling. Plos ONE. 2009; 4(9): e7124.
[4].  Fardeau, M., Tomé, F., & Simon, P. Muscle and nerve changes induced by perhexiline maleate in man and mice. Muscle & Nerve. 1979; 2(1): 24-36.

Chemical Properties

Cas No. 6724-53-4 SDF
别名 马来酸哌克昔林
化学名 2-(2,2-dicyclohexylethyl)-piperidine, 2Z-butenedioate
Canonical SMILES OC(/C=C\C(O)=O)=O.C1(CC(C2CCCCC2)C3CCCCC3)NCCCC1
分子式 C19H35N • C4H4O4 分子量 393.6
溶解度 ≤5mg/ml in ethanol;30mg/ml in DMSO;25mg/ml in dimethyl formamide 储存条件 Store at -20°C
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1 mM 2.5407 mL 12.7033 mL 25.4065 mL
5 mM 0.5081 mL 2.5407 mL 5.0813 mL
10 mM 0.2541 mL 1.2703 mL 2.5407 mL
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