Perhexiline maleate

Name: Perhexiline maleate
Brand: MedChemExpress
SKU: HY-B1334A
Rating: 4.5 (1 reviews)

Cat. No.: HY-B1334A Purity: 99.26%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Perhexiline maleate is an orally active CPT1 and CPT2 inhibitor that reduces fatty acid metabolism. Perhexiline maleate induces mitochondrial dysfunction and apoptosis in hepatic cells. Perhexiline maleate can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline maleate can be used in the research of cancers, and cardiovascular disease like angina.

For research use only. We do not sell to patients.

Perhexiline maleate Chemical Structure

CAS No. : 6724-53-4

Size	Price	Stock	Quantity
Solution
10 mM * 1 mL in Ethanol	USD 110	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 270	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 600	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Perhexiline maleate:

Perhexiline Get quote
Perhexiline-d₁₁ maleate Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 77 μM (Rat heart CPT 1), 148 μM (Rat liver CPT 1)^[1]

In Vitro

Perhexiline (5-25 μM, 2-6 h) maleate reduces cell viability in HepG2 cells^[2].
Perhexiline (5-25 μM, 2-6 h) maleate reduces cellular ATP content and Lactate dehydrogenase (LDH) release in HepG2 cells^[2].
Perhexiline (20 μM, 2 h) maleate activates caspase 3/7 in HepG2 cells^[2].
Perhexiline (5-25 μM, 4 h) maleate causes mitochondrial dysfunction in HepG2 cells^[2].
Perhexiline (5 μM, 48 h) maleate selectively induces massive apoptosis in CLL cells (high expression of CPT)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

In Vivo

Perhexiline (200 mg/kg, p.o., daily for 8 weeks) maleate reduces peripheral neural function in female DA rats^[4].
Perhexiline (80 mg/kg, oral gavage, for 3 days) maleate demonstrates anti-tumor activity in glioblastoma mouse model^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

Molecular Weight

393.56

Formula

C₂₃H₃₉NO₄

CAS No.

6724-53-4

Appearance

Solid

Color

White to off-white

SMILES

O=C(O)/C=C\C(O)=O.C1(CC(C2CCCCC2)C3CCCCC3)NCCCC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

Ethanol : 25 mg/mL (63.52 mM; ultrasonic and warming and heat to 60°C)

DMSO : 3.57 mg/mL (9.07 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (5.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.5 mg/mL (1.27 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.5 mg/mL (1.27 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.5 mg/mL (1.27 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.26%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (248 KB) LCMS (399 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[5]. Shiva Kant, et al. Perhexiline Demonstrates FYN-mediated Antitumor Activity in Glioblastoma. Mol Cancer Ther. 2020 Jul;19(7):1415-1422. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / Ethanol	1 mM	2.5409 mL	12.7045 mL	25.4091 mL	63.5227 mL
DMSO / Ethanol	5 mM	0.5082 mL	2.5409 mL	5.0818 mL	12.7045 mL
Ethanol	10 mM	0.2541 mL	1.2705 mL	2.5409 mL	6.3523 mL
	15 mM	0.1694 mL	0.8470 mL	1.6939 mL	4.2348 mL
	20 mM	0.1270 mL	0.6352 mL	1.2705 mL	3.1761 mL
	25 mM	0.1016 mL	0.5082 mL	1.0164 mL	2.5409 mL
	30 mM	0.0847 mL	0.4235 mL	0.8470 mL	2.1174 mL
	40 mM	0.0635 mL	0.3176 mL	0.6352 mL	1.5881 mL
	50 mM	0.0508 mL	0.2541 mL	0.5082 mL	1.2705 mL
	60 mM	0.0423 mL	0.2117 mL	0.4235 mL	1.0587 mL