Etomoxir, IC-0320381
Product Introduction
Carnitine palmitoyltransferase 1 (CPT1) is a rate-limiting enzyme on the outer mitochondrial membrane that controls the transport of long-chain fatty acids into the mitochondria for ¦Â-oxidation, a process central to cellular energy metabolism and implicated in metabolic disorders, inflammation, and cancer. Etomoxir ((R)-(+)-Etomoxir) is a cell-permeable, irreversible, and stereospecific inhibitor of CPT1a, with an IC50 of 5-20 nM for inhibiting fatty acid ¦Â-oxidation in rat liver. By blocking fatty acid transport into the mitochondria, Etomoxir shifts cellular energy reliance from fatty acid oxidation to glucose utilization. In rat heart H9c2 myoblastic cells, Etomoxir (1-80 µM) inhibits both CPT1 and DGAT activity. Beyond CPT1 inhibition, Etomoxir also acts as a PPAR¦Á agonist and disrupts CoA homeostasis, thereby inhibiting macrophage polarization. Historically developed in the 1980s by Byk Gulden Lomberg Chemische Fabrik GmbH, Etomoxir was initially investigated for treating metabolic disorders and has since been suggested as a potential therapeutic agent for heart failure.
Product Features
1. Potent CPT1a Inhibitor: Irreversible and stereospecific inhibition of carnitine palmitoyltransferase 1a with IC50 of 5-20 nM in rat liver.
2. Metabolic Reprogramming: Shifts cellular energy reliance from fatty acid oxidation to glucose utilization by blocking mitochondrial fatty acid transport.
3. Dual Enzyme Inhibition: Inhibits both CPT1 and diacylglycerol acyltransferase (DGAT) activity in cardiac myoblastic cells.
4. PPAR¦Á Agonist Activity: Acts as a peroxisome proliferator-activated receptor alpha agonist, contributing to transcriptional regulation of lipid metabolism.
5. Macrophage Modulation: Disrupts CoA homeostasis and inhibits macrophage polarization, with implications for inflammation and immunometabolism research.
Specifications
Size: Available in 10 mg, 25 mg, and 50 mg
CAS Number: 124083-20-1
Molecular Weight: 326.82
Molecular Formula: C17H23ClO4
Purity: ¡Ý99%
Solubility: DMSO: 100 mg/mL
Storage and Stability
Storage Conditions: In solvent, store at -80¡ãC for up to 6 months or -20¡ãC for up to 1 month. Protect from light and store under nitrogen.
Shelf Life: The product is stable as indicated when stored under recommended conditions. Avoid repeated freeze-thaw cycles and exposure to air.
Protocol (For Reference Only)
Important: Etomoxir is light-sensitive and oxygen-sensitive. Prepare stock solutions under inert gas and protect from light during handling and storage.
1. Stock Solution Preparation: Dissolve Etomoxir in anhydrous DMSO under nitrogen or argon atmosphere to prepare a concentrated stock solution (e.g., 10-100 mM), aliquot into single-use airtight vials, and store at -20¡ãC or -80¡ãC protected from light.
2. Working Solution Preparation: Immediately before use, dilute the DMSO stock solution into aqueous buffer or culture medium to the desired final concentration; typical working concentrations range from 1-100 µM depending on cell type and experimental endpoint.
3. Cellular Treatment: Add the working solution to cultured cells and incubate for the desired duration; for CPT1 inhibition studies, pretreatment for 30-60 minutes before metabolic assays is recommended.
4. Fatty Acid Oxidation Assays: Monitor metabolic shift by measuring oxygen consumption rate, fatty acid uptake, or assessing mitochondrial function using Seahorse or similar metabolic flux analyzers.
5. Analysis: Assess CPT1 inhibition by measuring palmitate oxidation rates, evaluate PPAR¦Á activation by reporter gene assays, or analyze macrophage polarization markers by flow cytometry and gene expression analysis.
Precautions
1. Protect from light and oxygen during handling and storage to prevent compound degradation.
2. Prepare fresh working solutions daily as the compound may lose activity upon prolonged storage in aqueous buffers or exposure to air.
3. Use appropriate vehicle controls in all experiments as DMSO concentrations above 0.1% may affect cellular metabolism and viability.
4. Etomoxir exhibits off-target effects including DGAT inhibition and PPAR¦Á agonism; confirm target specificity using appropriate controls and complementary approaches.
5. For research use only. Not for use in diagnostic or therapeutic procedures.
FAQ (Simplified)
Q1: What is the recommended starting concentration for in vitro CPT1 inhibition?
A1: For complete CPT1 inhibition in most cell types, 40-80 µM is commonly used. However, partial inhibition can be achieved at lower concentrations (1-10 µM). Titration experiments are recommended to determine optimal conditions for specific applications.
Q2: How should I store Etomoxir to maintain stability?
A2: Etomoxir is sensitive to light and oxygen. Prepare stock solutions in anhydrous DMSO under inert gas (nitrogen or argon), aliquot into airtight vials, and store at -80¡ãC for long-term storage or -20¡ãC for short-term use. Avoid repeated freeze-thaw cycles.
Q3: Does Etomoxir affect other metabolic pathways?
A3: Yes. In addition to CPT1 inhibition, Etomoxir inhibits DGAT activity, acts as a PPAR¦Á agonist, and disrupts CoA homeostasis. These off-target effects should be considered when interpreting experimental results, particularly in macrophage and cardiac studies.
Q4: Can Etomoxir be used in vivo?
A4: Yes. Etomoxir has been administered to rodents at doses ranging from 10-50 mg/kg via intraperitoneal or oral routes for metabolic studies. Optimize dosing and vehicle based on specific experimental requirements and consult literature for established protocols.
Disclaimer
1. For Research Use Only. Not for use in diagnostic or therapeutic procedures.
2. Due to the variable nature of biological research, optimization of conditions using a small-scale pilot experiment is strongly recommended before processing valuable samples.
3. This warranty is limited to the replacement of the product. The manufacturer assumes no liability for incidental or consequential damages, including loss of samples or data.
4. Wear appropriate protective clothing and gloves when handling this product.
Ordering Information
Catalog Number: IC-0320381
Product Name: Etomoxir
Size: 10 mg / 25 mg / 50 mg
Price:
10 mg: CNY ¥1700.00 / USD $170.00 / EUR €204.00 / JPY ¥30600.00
25 mg: CNY ¥2800.00 / USD $280.00 / EUR €336.00 / JPY ¥50400.00
50 mg: CNY ¥4800.00 / USD $480.00 / EUR €576.00 / JPY ¥86400.00
2023 Version
