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Purity: ≥98%
Etomoxir is a novel, potent and irreversible (covalent) inhibitor of carnitine palmitoyltransferase-1 (CPT-1) on the outer face of the inner mitochondrial membrane. It inhibits β-oxidation in mitochondria; shown to inhibit cardiolipin biosynthesis from exogenous fatty acid in H9c2 cells. Etomoxir has also been identified as a direct agonist of PPARα. Etomoxir is a compound that binds irreversibly to the catalytic site of CPT-1 inhibiting its activity, but also upregulates fatty acid oxidation enzymes.
| ln Vitro |
When etomoxir binds irreversibly to CPT-1's catalytic site, it inhibits CPT-1's activity while simultaneously increasing transplantation oxidase. Etomoxir was created as a probe for the outer mitochondrial membrane-localized mitochondrial carnitine scaffold amplification enzyme-1 (CPT-1). Etomoxir stimulates DNA synthesis and myocardial development in the myocardium by acting as an oxisome proliferator. Consequently, etomoxan is regarded as a PPARalpha agonist in addition to a CPT1 [1]. Etomoxir has been proposed as a target for activation of cardiac mutations. It is a member of the ethylene oxide kinase carnitine template transferase I family. Carnitine template transferase I activity is irreversibly transcribed upon activation of Etomoxir therapy. Consequently, there is a decrease in base import as mitochondria and beta-oxidation, leading to an increase in cytoplasmic accumulation and oxidation. Etomoxir's long delays (24 hours) have even distinct impacts on the expression of enzymes [2].
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| ln Vivo |
Etomoxir is a transcription factor that is involved in free equilibrium (FFA) oxidation and is linked to the important enzyme CPT1. Further supporting the direct response of P53 and Bax, as well as the role of FAO-mediated catalytic ROS production in the db/db model, is the fact that P53 directly responds to Bax, and Bax is blocked by etomoxir [3]. At a dose of 20 mg/kg body weight, etomoxir was injected once daily for eight days, resulting in a 44% reduction in specific CPT-I activity. The catalyst CPT-I activity was 44% lower in the catalyst treated with etomoxir. Lewis's blood glucose levels remained unchanged after 8 days of treatment with 20 mg/kg Etomoxir, in line with previous Etomoxir feeding trials. Similarly, etomoxir feeding had no effect on harvest mass in the hindlimb or on general growth traits like weight gain. However, in those treated with etomoxir, both liver and heart mass grew significantly by 11% [4].
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| References |
[1]. Rupp H, et al. The use of partial fatty acid oxidation inhibitors for metabolic therapy of angina pectoris and heart failure. Herz. 2002 Nov;27(7):621-36.
[2]. Xu FY, et al. Etomoxir mediates differential metabolic channeling of fatty acid and glycerol precursors into cardiolipin in H9c2 cells. J Lipid Res. 2003 Feb;44(2):415-23. [3]. Li J, et al. FFA-ROS-P53-mediated mitochondrial apoptosis contributes to reduction of osteoblastogenesis and bone mass in type 2 diabetes mellitus. Sci Rep. 2015 Jul 31;5:12724. [4]. Luiken JJ, et al. Etomoxir-induced partial carnitine palmitoyltransferase-I (CPT-I) inhibition in vivo does not alter cardiac long-chain fatty acid uptake and oxidation rates. Biochem J. 2009 Apr 15;419(2):447-55. [5]. O'Connor RS, et al. The CPT1a inhibitor, etomoxir induces severe oxidative stress at commonly used concentrations. Sci Rep. 2018 Apr 19;8(1):6289 |
| Molecular Formula |
C17H23CLO4
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|---|---|
| Molecular Weight |
326.82
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| Exact Mass |
326.1285
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| CAS # |
124083-20-1
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| Related CAS # |
Etomoxir sodium salt;828934-41-4
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| SMILES |
O=C([C@]1(CCCCCCOC2=CC=C(Cl)C=C2)OC1)OCC
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| Chemical Name |
Ethyl (2R)-2-[6-(4-chlorophenoxy)hexyl]oxirane-2-carboxylate
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| Synonyms |
(R)-(+)-Etomoxir B 807-54 B80754 B-80754B807-54 B-807-54 B 80754
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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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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) |
DMSO : ~100 mg/mL (~305.98 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 3.5 mg/mL (10.71 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 35.0 mg/mL clear DMSO 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: ≥ 3.5 mg/mL (10.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 35.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 2.5 mg/mL (7.65 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Solubility in Formulation 4: 10 mg/mL (30.60 mM) in 0.5% Methylcellulose/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0598 mL | 15.2989 mL | 30.5979 mL | |
| 5 mM | 0.6120 mL | 3.0598 mL | 6.1196 mL | |
| 10 mM | 0.3060 mL | 1.5299 mL | 3.0598 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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