Etomoxir sodium salt

Catalog No.S8244 Batch:S824403

Technical Data

Formula	C₁₅H₁₈ClO₄.Na
Molecular Weight	320.74	CAS No.	828934-41-4
Solubility (25°C)*	In vitro	DMSO	64 mg/mL (199.53 mM)
		Water	64 mg/mL (199.53 mM)
		Ethanol	8 mg/mL (24.94 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Etomoxir sodium salt ((R)-(+)-Etomoxir sodium salt) is an irreversible inhibitor of carnitine palmitoyltransferase-1 (CPT-1) on the outer face of the inner mitochondrial membrane. Etomoxir enhances palmitate-induced cell apoptosis.

Targets

CPT-1 ^[1]

PPARα ^[1]

In vitro

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. Transcriptional effects of etomoxir could be due to 1. shift in energy metabolism with increased glucose utilization and 2. PPARalpha activation^[1]. Etomoxir reduces pro-inflammatory cyokine production and increases apoptosis of MOG specific T cells^[2]. Etomoxir has been shown to decrease oxygen consumption rates (OCRs) and impair ATP and NADPH production in the pediatric glioblastoma cell line SF188^[3].

In vivo

Etomoxir has a protective action on the ischemia/reperfusion injury of the kidney similarly to an established PPARalpha agonist. It has been developed for treating non-insulindependent diabetes mellitus. Etomoxir increases the functional recovery of fatty acid perfused ischemic rat hearts which is unrelated to changes in levels of long-chain acylcarnitines and is attributed to an increased glucose use. A chronic treatment of rats with etomoxir increases the SR Ca2+-ATPase activity, the Ca2+ uptake rate, the number of active Ca2+ pumps E~P, the SERCA2 protein and the SERCA2 mRNA abundance of the heart. At a low dosage, etomoxir has a selective influence on the rate of contraction and relaxation of overloaded hearts. Etomoxir, in the liver can act as peroxisomal proliferator, increasing DNA synthesis and liver growth^[1]. Etomoxir-treated mice displays a reduced immune cell infiltration in the CNS with few macrophages, activated microglia, or T cells present. Etomoxir reduces inflammation and demyelination in the CNS of treated mice^[2]. Inhibition of fatty acid oxidation by etomoxir prolongs survival time in a syngeneic mouse model of malignant glioma and slow tumor growth. Emergence and progression of glioma are delayed upon treatment with the investigational drug etomoxir. Etomoxir has already been tested in phase I/II clinical trials for treating moderate congestive heart failure; this trial is discontinued because 4 patients (of 226 taking the drug) developed unacceptably high liver transaminase levels upon treatment, and the risk of such drastic side effects is deemed sufficient to negate the potential benefit of this drug for these patients^[3].

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines Splenocytes Concentrations 100 μM Incubation Time 72 h Method C57BL/6 mice are immunized with 200 μg MOG_35-55 peptide s.c., and 14 days later splenocytes are isolated and cultured at a concentration of 6×10_⁶ cells/ml in DMEM containing high (4.5 g/L) or low (1 g/L) glucose, 10% FBS 50 μg/ml MOG peptide, and 25 ng/ml IL-12 (R&D systems, Minneapolis, MN) in the presence of vehicle or 100 μM etomoxir. 72 hours later cells are harvested for APO-BrdU staining and supernatants collected for IL-4, IL-17 and IFN-γ ELISA. (MOG:myelin oligodendrocyte glycoprotein)
Animal Study:^{^[2]}	Animal Models C57BL6/J mice Dosages 15 mg/kg Administration i.p.

Cell Assay:^{^[2]}

Cell lines
Splenocytes
Concentrations
100 μM
Incubation Time
72 h
Method
C57BL/6 mice are immunized with 200 μg MOG_35-55 peptide s.c., and 14 days later splenocytes are isolated and cultured at a concentration of 6×10_⁶ cells/ml in DMEM containing high (4.5 g/L) or low (1 g/L) glucose, 10% FBS 50 μg/ml MOG peptide, and 25 ng/ml IL-12 (R&D systems, Minneapolis, MN) in the presence of vehicle or 100 μM etomoxir. 72 hours later cells are harvested for APO-BrdU staining and supernatants collected for IL-4, IL-17 and IFN-γ ELISA. (MOG:myelin oligodendrocyte glycoprotein)

Animal Study:^{^[2]}

Animal Models
C57BL6/J mice
Dosages
15 mg/kg
Administration
i.p.

References

Customer Product Validation

: Data from [Data independently produced by , , Cancer Lett, 2018, 442:40-52]

: Data from [Data independently produced by , , Med Sci Monit, 2018, 24:1484-1492]

: Data from [Data independently produced by , , Med Sci Monit, 2018, 24: 1484-1492]

: Data from [Data independently produced by , , Lymphatic Research and BiologyVol, 2018, 16(1). https://doi.org/10.1089/lrb.2017.0033]

Selleck's Etomoxir sodium salt has been cited by 48 publications

Extracellular matrix stiffness as an energy metabolism regulator drives osteogenic differentiation in mesenchymal stem cells [ Bioact Mater, 2024, 35:549-563]	PubMed: 38434800
Small molecules targeting selective PCK1 and PGC-1α lysine acetylation cause anti-diabetic action through increased lactate oxidation [ Cell Chem Biol, 2024, 31(10):1772-1786.e5]	PubMed: 39341205
PIM1 drives lipid droplet accumulation to promote proliferation and survival in prostate cancer [ Oncogene, 2024, 43(6):406-419]	PubMed: 38097734
Monocyte and macrophage profiles in patients with inherited long-chain fatty acid oxidation disorders [ Biochim Biophys Acta Mol Basis Dis, 2024, 1871(1):167524]	PubMed: 39307292
Targeting metabolic adaptive responses induced by glucose starvation inhibits cell proliferation and enhances cell death in osimertinib-resistant non-small cell lung cancer (NSCLC) cell lines [ Biochem Pharmacol, 2024, S0006-2952(24)00144-8]	PubMed: 38522556
NINJ1 regulates ferroptosis via xCT antiporter interaction and CoA modulation [ bioRxiv, 2024, 2024.02.22.581432]	PubMed: 38464226
Immuno-metabolic dendritic cell vaccine signatures associate with overall survival in vaccinated melanoma patients [ Nat Commun, 2023, 10.1038/s41467-023-42881-4]	PubMed: 37938561
Restoration of CPT1A-mediated fatty acid oxidation in mesothelial cells protects against peritoneal fibrosis [ Theranostics, 2023, 13(13):4482-4496]	PubMed: 37649600
Restoration of CPT1A-mediated fatty acid oxidation in mesothelial cells protects against peritoneal fibrosis [ Theranostics, 2023, 10.7150/thno.84921]	PubMed: 37649600
Perturbation of Copper Homeostasis Sensitizes Cancer Cells to Elevated Temperature [ Int J Mol Sci, 2023, 25(1)423]	PubMed: 38203594

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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