Home Metabolism CPT inhibitor - Transferase inhibitor - Apoptosis related activator Etomoxir sodium salt For research use only.

Etomoxir sodium salt

Synonyms: (R)-(+)-Etomoxir sodium salt

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.

Etomoxir sodium salt Chemical Structure

Etomoxir sodium salt Chemical Structure

CAS No. 828934-41-4

Purity & Quality Control

Products often used together with Etomoxir sodium salt

BPTES

Etomoxir inhibits CPT1 and BPTES blocks glutaminase GLS1 in tumor-bearing mice.

Corbet C, et al. Cell Metab. 2016 Aug 9;24(2):311-23.

UK 5099

Etomoxir and UK5099 synergistically inhibit mitochondrial fusion dynamics when pre-incubated for 1 h prior to the beginning of the fusion experiment in differentiated PC12 cells.

O'Hara D, et al. Front Mol Neurosci. 2019 Sep 18;12:219.

Alisertib (MLN8237)

Etomoxir and Alisertib combination use induces tumor regression and prolongs overall survival of the mice.

Marocchi F, et al. J Invest Dermatol. 2023 Mar 31;S0022-202X(23)01952-8.

Trimetazidine

Etomoxir reduces the toxic effect of trimetazidine in quiescence-induced cancer cells.

Ortmayr K, et al. Mol Syst Biol. 2022 Sep;18(9):e10716.

Etomoxir sodium salt Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KB cells Cytotoxicity assay Cytotoxicity in human KB cells, IC50=2.76 μM 21504156
U251 Growth inhibiton assay 50 μM 72-h treatments have slight growth inhibitory effects 30574020
U87 Growth inhibiton assay 50 μM 72-h treatments have slight growth inhibitory effects 30574020
U373-U Growth inhibiton assay 50 μM 72-h treatments have slight growth inhibitory effects 30574020
MCF-7 cells Function assay 0–200 μM 4 h in db-cAMP-exposed cells ETO caused a metabolic imbalance 30981740
HepG2 cells Function assay 24 h Etomoxir significantly inhibits palmitate metabolism with an IC50 in the nanomolar range. 29740314
Click to View More Cell Line Experimental Data

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
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].
Cell Research Cell lines Splenocytes
Concentrations 100 μM
Incubation Time 72 h
Method

C57BL/6 mice are immunized with 200 μg MOG35-55 peptide s.c., and 14 days later splenocytes are isolated and cultured at a concentration of 6×106 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)
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-ERK / p-p38 / p-JNK / p-FoxO4 p21 / FoxO1 / FoxO3a p-mTOR(S2448) / mTOR / p-S6K(T389) / p-4EBP1 / p-BAD(S112) / cleaved PARP p-ACC2 / p-AMPK / AMPK 26716645
In Vivo
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].
Animal Research Animal Models C57BL6/J mice
Dosages 15 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 320.74 Formula

C15H18ClO4.Na
CAS No. 828934-41-4 SDF Download Etomoxir sodium salt SDF
Smiles C1C(O1)(CCCCCCOC2=CC=C(C=C2)Cl)C(=O)[O-].[Na+]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 64 mg/mL ( (199.53 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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