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Etomoxir sodium salt CPT-1 inhibitor

Name: Etomoxir sodium salt
Brand: Selleck Chemicals
SKU: S8244
Availability: InStock
Rating: 5 (51 reviews)

Cat.No.S8244

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.

Chemical Structure

Molecular Weight: 320.74

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.87%

99.87

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Related Targets	P450 (e.g. CYP17) Dehydrogenase PDE phosphatase PPAR HSP (HSP90) Vitamin Transferase Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase Serine/threonin kinase Lipoxygenase Phospholipase (e.g. PLA) Retinoid Receptor DPP ACE Peroxidases Fatty Acid Synthase FXR HMG-CoA Reductase Carbonic Anhydrase Lipase Decarboxylase DHFR IDO/TDO Hydroxylase PCSK9 OXPHOS ROR
Related Products	Perhexiline maleate

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	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

Chemical Information, Storage & Stability

Molecular Weight	320.74	Formula	C₁₅H₁₈ClO₄.Na	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	828934-41-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	(R)-(+)-Etomoxir sodium salt			Smiles	C1C(O1)(CCCCCCOC2=CC=C(C=C2)Cl)C(=O)[O-].[Na+]

Solubility

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.000mg/ml (9.35mM)	Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.200mg/ml (9.98mM)	Taking the 1 mL working solution as an example, add 50 μL 64 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	CPT-1 ^[1] PPARα ^[1]
In vitro	Etomoxir sodium salt has also been identified as a direct agonist of PPARα. This compound 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]. It 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 sodium salt 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. This compound 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 this chemical 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, it has a selective influence on the rate of contraction and relaxation of overloaded hearts. This compound, 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. It reduces inflammation and demyelination in the CNS of treated mice^[2]. Inhibition of fatty acid oxidation by this chemical 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. It 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].
References	https://pubmed.ncbi.nlm.nih.gov/12439634/ https://pubmed.ncbi.nlm.nih.gov/22355598/ https://pubmed.ncbi.nlm.nih.gov/27365097/

Applications

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

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