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| 25mg |
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Purity: ≥98%
Etomoxir sodium salt, the sodium salt form of etomoxir, is an irreversible 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 |
In H9c2 cells, etomoxir facilitates the distinct metabolic channeling of fatty acid and glycerol precursors into cardiolipin[2]. Although etomoxir reduces the incorporation of [1-14C]palmitic acid or [1-14C]oleic acid into cardiolipin, it has no effect on the activity of the enzymes involved in the biosynthesis and remodeling of cardiolipin[2]. Cardiolipin's incorporation of [1,3-3H]glycerol is increased by etomoxir. The process involves a 33% rise in glycerol kinase activity, which causes an increase in glycerol flux via the cardiolipin biosynthesis de novo pathway [2].
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| ln Vivo |
Etomoxir suppresses the reduction of BMSCs-differentiated osteoblasts and significantly inhibits the decrease of bone mineral density (BMD) and bone breaking strength in mice fed high fat (HF) and db/db diets[3]. In mice fed HF and db/db, etopoxir inhibits the increase in mitochondrial ROS generation in osteoblasts and mice[3]. The in vivo partial inhibition of carnitine palmitoyltransferase-I (CPT-I) caused by etomoxir does not change the rates of cardiac long-chain fatty acid uptake and oxidation[4].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: Rat heart H9c2 myoblastic cells Tested Concentrations: 1-80 μM Incubation Duration: 2 hrs (hours) Experimental Results: decreased the incorporation of [1-14C]fatty acids into CL and PtdGro in H9c2 cardiac myoblast cells but did not affect total incorporation of radioactivity into these cells. |
| Animal Protocol |
Animal/Disease Models: 80 male C57BLKS/J lar-Leprdb/db mice[3]
Doses: 1 mg/kg Route of Administration: Intraperitoneally injected; twice every week Experimental Results: Serum alkaline phosphatase was increased in db/db mice, which event was Dramatically suppressed by Etomoxir. Serum level of osteocalcin, a marker of bone formation, was decreased in db/db mice and Etomoxir markedly inhibited the reduction of osteocalcin. Serum tartrate-resistant acid phosphatase was elevated in db/db mice which phenomenon was Dramatically suppressed by Etomoxir. Animal/Disease Models: Rats[4] Doses: 20 mg/kg Route of Administration: Injected daily; for 8 days Experimental Results: Etomoxir-treated rats displayed a 44% decreased cardiac CPT-I activity. |
| References |
[1]. Roddy S O'Connor, et al. The CPT1a inhibitor, etomoxir induces severe oxidative stress at commonly used concentrations.Sci Rep. 2018 Apr 19;8(1):6289.
[2]. Fred Y Xu,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]. Jun Li, 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]. Joost J F P Luiken, 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. |
| Molecular Formula |
C15H18CLO4.NA
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| Molecular Weight |
320.74
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| CAS # |
828934-41-4
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| Related CAS # |
Etomoxir;124083-20-1
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| SMILES |
ClC1=CC=C(OCCCCCC[C@@]2(CO2)C([O-])=O)C=C1.[Na+]
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| Chemical Name |
(2R)-2-[6-(4-chlorophenoxy)hexyl]-2-oxiranecarboxylic acid monosodium salt
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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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (7.79 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 sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.79 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. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 3.33 mg/mL (10.38 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1178 mL | 15.5890 mL | 31.1779 mL | |
| 5 mM | 0.6236 mL | 3.1178 mL | 6.2356 mL | |
| 10 mM | 0.3118 mL | 1.5589 mL | 3.1178 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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