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| 5mg |
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| 10mg |
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| 25mg |
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Perhexiline maleate is a potent anti-anginal metabolic modulator, inhibiting the mitochondrial enzyme carnitine palmitoyltransferase CPT-1 and to a lesser extent CPT-2. This causes a shift in myocardial substrate utilisation from long chain fatty acids to carbohydrates, resulting in increased glucose and lactate utilization and increased ATP production for the same O2 consumption as before and consequently increases myocardial efficiency.
| ln Vitro |
HepG2 cell viability is decreased by perhexiline (5–25 μM, 2–6 h)maleate [2]. In HepG2 cells, perhexiline (5–25 μM, 2–6 h)maleate lowers the amount of ATP and resting dehydrogenase (LDH). In HepG2 cells, perhexiline (20 μM, 2 h)maleate activates caspase 3/7 [2]. In HepG2 cells, perhexiline (5–25 μM, 4 h)maleate promotes the induction of mitochondrial function [2]. In CLL cells, the maleate route of perhexiline (5 μM, 48 h) causes bulk electrophoresis, or high expression of CPT [3].
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| ln Vivo |
Perhexiline (200 mg/kg, lateral, once daily for 8 weeks) maleate decreases DA-related peripheral nerve function in females [4]. Perhexiline (80 mg/kg, side wall gavage, 3 consecutive days) maleate In-gel tumor
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: HepG2 cells Tested Concentrations: 5, 10, 15, 25 μM Incubation. Incubation Duration: 2, 4, 6 hrs (hours) Experimental Results: Induction of time- and concentration-dependent cytotoxicity in hepatocytes. Western Blot Analysis [2] Cell Types: HepG2 Cell Tested Concentrations: 5, 10, 15, 25 μM Incubation Duration: 2 h Experimental Results: Bcl-2 and Mcl-1 levels diminished, and Bad levels increased. |
| Animal Protocol |
Animal/Disease Models: orthotopic glioblastoma mouse model [5]
Doses: 80 mg/kg Route of Administration: po (oral gavage) , for 3 days. Demonstrated anti-activity in blastoid tumor models [5]. Experimental Results: diminished tumor size (magnetic resonance imaging) and improved overall survival. |
| 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. [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. [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. [5]. Shiva Kant, et al. Perhexiline Demonstrates FYN-mediated Antitumor Activity in Glioblastoma. Mol Cancer Ther. 2020 Jul;19(7):1415-1422. |
| Molecular Formula |
C23H39NO4
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|---|---|
| Molecular Weight |
393.56006
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| CAS # |
6724-53-4
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| Related CAS # |
Perhexiline;6621-47-2;Perhexiline-d11 maleate
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| SMILES |
C1CCC(CC1)C(CC2CCCCN2)C3CCCCC3.C(=CC(=O)O)C(=O)O
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| InChi Key |
JDZOTSLZMQDFLG-BTJKTKAUSA-N
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| InChi Code |
InChI=1S/C19H35N.C4H4O4/c1-3-9-16(10-4-1)19(17-11-5-2-6-12-17)15-18-13-7-8-14-20-185-3(6)1-2-4(7)8/h16-20H,1-15H21-2H,(H,5,6)(H,7,8)/b2-1-
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| Chemical Name |
2-(2,2-dicyclohexylethyl)piperidine maleate
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| Synonyms |
Pexid CCRIS
5491 2-(2,2-Dicyclohexylethyl)piperidine maleate perhexiline maleate
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
Ethanol : ~25 mg/mL (~63.52 mM)
DMSO : ~3.57 mg/mL (~9.07 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (5.08 mM) (saturation unknown) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear EtOH stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 0.5 mg/mL (1.27 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.5 mg/mL (1.27 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: (saturation unknown) in (add these co-solvents sequentially from left to right, and one by one), |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5409 mL | 12.7045 mL | 25.4091 mL | |
| 5 mM | 0.5082 mL | 2.5409 mL | 5.0818 mL | |
| 10 mM | 0.2541 mL | 1.2705 mL | 2.5409 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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