| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 100mg |
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| Targets |
The primary target of Perhexiline Maleate is carnitine palmitoyltransferase 1 (CPT1), the rate-limiting enzyme in mitochondrial fatty acid oxidation. CPT1 catalyzes the transfer of long-chain fatty acyl-CoA to carnitine, allowing fatty acids to enter the mitochondria for β-oxidation. Perhexiline Maleate is a potent inhibitor of CPT1 with IC₅₀ values of 77 μM and 148 μM for rat heart and liver CPT1, respectively. It also inhibits CPT2 to a lesser extent. By inhibiting CPT1/2, the compound reduces fatty acid metabolism and shifts myocardial substrate utilization towards carbohydrates.
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| 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].
In vitro, Perhexiline Maleate inhibits CPT1 with IC₅₀ values of 77 μM and 148 μM for rat heart and liver CPT1, respectively. It also inhibits CPT2 to a lesser extent. The compound promotes HER3 ablation through receptor internalization and inhibits tumor growth. By reducing fatty acid metabolism, Perhexiline Maleate shifts substrate utilization from long-chain fatty acids to carbohydrates. |
| 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
In vivo, Perhexiline Maleate is an orally active anti-anginal agent that improves myocardial efficiency by shifting substrate utilization from fatty acids to carbohydrates. It has been used clinically as an anti-anginal drug since the 1970s. The compound also promotes HER3 ablation through receptor internalization and inhibits tumor growth. Its oral bioavailability makes it suitable for convenient administration in clinical settings. |
| Enzyme Assay |
For CPT1 inhibitors, standard cell-free assays involve measuring the transferase activity of CPT1 using radiolabeled palmitoyl-CoA and L-carnitine. The compound is incubated with the enzyme and substrates, and the formation of radiolabeled palmitoylcarnitine is measured by scintillation counting to determine IC₅₀ values.
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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. For CPT1 inhibitors, standard cellular assays involve treatment of hepatocytes or cardiomyocytes with the test compound. Fatty acid oxidation is measured by the oxidation of radiolabeled fatty acids (e.g., [¹⁴C]-palmitate) to ¹⁴CO₂. Cellular ATP levels, oxygen consumption, and substrate utilization are assessed. |
| 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. For in vivo evaluation of CPT1 inhibitors, standard animal models include models of myocardial ischemia, heart failure, and metabolic disorders. The compound is typically administered orally, and endpoints include myocardial efficiency, fatty acid oxidation, glucose utilization, and cardiac function. Perhexiline Maleate has been used clinically as an anti-anginal drug. |
| ADME/Pharmacokinetics |
Perhexiline Maleate is an orally active inhibitor of CPT1 and CPT2. It has a molecular weight of 393.56 and formula C₂₃H₃₉NO₄. The compound is a prophylactic antianginal agent. It has been used clinically since the 1970s. Comprehensive PK studies have been conducted as part of its clinical development.
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| Toxicity/Toxicokinetics |
Perhexiline Maleate has been used clinically as an anti-anginal drug since the 1970s. It has a well-established safety profile, though it can cause hepatotoxicity and peripheral neuropathy in some patients due to genetic polymorphisms in CYP2D6 affecting its metabolism. The compound is also a calcium channel inhibitor. Comprehensive toxicological evaluation has been conducted as part of its clinical development.
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| References | |
| Additional Infomation |
Perhexiline Maleate is a potent anti-anginal metabolic modulator that inhibits CPT1 and CPT2. It has IC₅₀ values of 77 μM and 148 μM for rat heart and liver CPT1, respectively. The compound shifts myocardial substrate utilization from fatty acids to carbohydrates. It has the molecular formula C₂₃H₃₉NO₄. Perhexiline Maleate is an approved drug for angina pectoris.
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| Molecular Formula |
C23H39NO4
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|---|---|
| Molecular Weight |
393.56006
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| Exact Mass |
393.288
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| Elemental Analysis |
C, 70.19; H, 9.99; N, 3.56; O, 16.26
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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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| PubChem CID |
5284439
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| Appearance |
White to off-white solid powder
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| Boiling Point |
574.1ºC at 760 mmHg
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| Melting Point |
181-183ºC
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| Flash Point |
301ºC
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| LogP |
5.336
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
364
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(O)/C=C\C(O)=O.C1(CC(C2CCCCC2)C3CCCCC3)NCCCC1
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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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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
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| 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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