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Perhexiline (maleate)

Catalog No.GC15257

CPT1 and CPT2 inhibitor

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Perhexiline (maleate) Chemical Structure

Cas No.: 6724-53-4

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1mg
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5mg
$84.00
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10mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

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.

Background

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
Chemical Name 2-(2,2-dicyclohexylethyl)-piperidine, 2Z-butenedioate
Canonical SMILES OC(/C=C\C(O)=O)=O.C1(CC(C2CCCCC2)C3CCCCC3)NCCCC1
Formula C19H35N • C4H4O4 M.Wt 393.6
Solubility ≤5mg/ml in ethanol;30mg/ml in DMSO;25mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
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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Average Rating: 5 ★★★★★ (Based on Reviews and 4 reference(s) in Google Scholar.)

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