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Etomoxir

Catalog No.GC16736

Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a). Etomoxir inhibits fatty acid oxidation (FAO) and palmitate oxidation via CPT-1a.

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Etomoxir Chemical Structure

Cas No.: 124083-20-1

Size Price Stock Qty
10mM (in 1mL DMSO)
$79.00
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5mg
$72.00
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10mg
$135.00
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25mg
$234.00
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50mg
$323.00
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100mg
$504.00
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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 3 publications

Description of Etomoxir

Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a). Etomoxir inhibits fatty acid oxidation (FAO) and palmitate oxidation via CPT-1a[1].

T cells cultured in a low-glucose medium in the presence of Etomoxir (100μM) significantly reduce interferon-gamma (IFN-γ) production and do not promote T-helper 2 (Th2)-related cytokine IL-4 production, while Etomoxir does not affect T cells cultured in the high-glucose medium[2]. Etomoxir (500μM) can significantly inhibit FAO in A549 and A549T cells. Etomoxir at 500μM or 1mM can significantly increase the sensitivity of paclitaxel-resistant cells (A549T) to paclitaxel[3].

In experimental autoimmune encephalomyelitis (EAE) mice, Etomoxir (15mg/kg) reduces inflammatory responses, immune cell infiltration in the central nervous system (CNS), as well as inflammation and demyelination in the CNS[2]. In C57BLKS/J lar-Leprdb/db and high-fat (HF)-fed mice, Etomoxir (1mg/kg) significantly reduces the decrease in bone mineral density (BMD) and bone-breaking strength and inhibits the decrease in osteoblasts differentiated from bone marrow stromal cells (BMSCs)[4].

References:
[1] Rupp H, et al. The use of partial fatty acid oxidation inhibitors for metabolic therapy of angina pectoris and heart failure. Herz. 2002 Nov;27(7):621-36.
[2] Shriver L P, Manchester M. Inhibition of fatty acid metabolism ameliorates disease activity in an animal model of multiple sclerosis[J]. Scientific Reports, 2011, 1(1): 79.
[3] Li J, Zhao S, Zhou X, et al. Inhibition of lipolysis by mercaptoacetate and etomoxir specifically sensitizes drug-resistant lung adenocarcinoma cells to paclitaxel[J]. PloS one, 2013, 8(9): e74623.
[4] Li J, He W, Liao B, et al. FFA-ROS-P53-mediated mitochondrial apoptosis contributes to the reduction of osteoblastogenesis and bone mass in type 2 diabetes mellitus[J]. Scientific Reports, 2015, 5(1): 12724.

Protocol of Etomoxir

Cell experiment [1]:

Cell lines

Rat heart H9c2 myoblastic cells

Preparation Method

H9c2 cells were preincubated with 1–80μM Etomoxir for 2h and incubated with 0.1mM [1-14C]oleic acid bound to albumin for 2h, and radioactivity incorporated into cardiolipin (CL) determined.

Reaction Conditions

1-80μM; 2h

Applications

In rat cardiac H9c2 myoblasts, Etomoxir reduced [1-14C]oleic acid incorporation into phosphatidylglycerol (PtdGro) and cardiolipin (CL) in a concentration-dependent manner and increased [1,3-3H]glycerol incorporation into CL.

Animal experiment [2]:

Animal models

Experimental autoimmune encephalomyelitis (EAE) mice model

Preparation Method

EAE was induced with a peptide from myelin oligodendrocyte glycoprotein (MOG35–55) and mice were administered Etomoxir.

Dosage form

15mg/kg, On days 8 and 15 after EAE induction, i.p.

Applications

Etomoxir treatment reduced inflammatory responses and immune cell infiltration in the central nervous system of EAE mice.

References:
[1] Xu FY1, Taylor WA, Hurd JA, 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. Epub 2002 Nov 4.
[2] Shriver LP1, Manchester M. Inhibition of fatty acid metabolism ameliorates disease activity in an animal model of multiple sclerosis. Sci Rep. 2011;1:79.

Chemical Properties of Etomoxir

Cas No. 124083-20-1 SDF
Chemical Name ethyl (2R)-2-[6-(4-chlorophenoxy)hexyl]oxirane-2-carboxylate
Canonical SMILES CCOC(=O)C1(CO1)CCCCCCOC2=CC=C(C=C2)Cl
Formula C17H23ClO4 M.Wt 326.82
Solubility ≥ 32.7 mg/mL in DMSO, ≥ 109.6 mg/mL in EtOH, ≥ 48.3 mg/mL in Water with gentle warming Storage Store at -20°C, protect from light, stored under nitrogen
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Etomoxir

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.0598 mL 15.2989 mL 30.5979 mL
5 mM 0.612 mL 3.0598 mL 6.1196 mL
10 mM 0.306 mL 1.5299 mL 3.0598 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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