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Cat. No.: HY-50202 Purity: 99.40%
Handling Instructions

Etomoxir is a potent inhibitor of carnitine palmitoyltransferase-I (CPT-1).

For research use only. We do not sell to patients.
Etomoxir Chemical Structure

Etomoxir Chemical Structure

CAS No. : 124083-20-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 92 In-stock
5 mg USD 84 In-stock
10 mg USD 144 In-stock
50 mg USD 504 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Other Forms of Etomoxir:

    Etomoxir purchased from MCE. Usage Cited in: Oncotarget. 2016 Oct 11;7(41):67071-67086.

    MDA-MB-453 cells are treated as indicated for 2 days and subjected to immunoblotting. Combination treatments using non-saturating doses of Etomoxir and MTI-31 or Rapamycin results in an enhanced growth suppression in MDA-MB-453 cells, which is not readily observed in MDA-MB-231 cells, correlating a nearly complete suppression of cyclin D1 and c-Myc level in MDA-MB-453 cells under the combination treatments.

    Etomoxir purchased from MCE. Usage Cited in: Redox Biol. 2018 Apr 18;17:180-191.

    MDA-MB-231 cells are cultured in poly-HEMA coated dishes and treated with Compound C or GL-V9 for 36 h. The expression of AMPK and p-AMPK in Compound C treated cells are assayed by Western blotting.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References


    Etomoxir is a potent inhibitor of carnitine palmitoyltransferase-I (CPT-1).

    IC50 & Target


    In Vitro

    Etomoxir binds irreversibly to the catalytic site of CPT-1 inhibiting its activity, but also upregulates fatty acid oxidation enzymes. Etomoxir is developed as an inhibitor of the mitochondrial carnitine palmitoyltransferase-1 (CPT-1) located on the outer mitochondrial membrane. Etomoxir, in the liver can act as peroxisomal proliferator, increasing DNA synthesis and liver growth. Thus, etomoxir, in addition of being a CPT1 inhibitor could be considered as a PPARalpha agonist[1]. Etomoxir is a member of the oxirane carboxylic acid carnitine palmitoyl transferase I inhibitors and has been suggested as a therapeutic agent for the treatment of heart failure. Acute Etomoxir treatment irreversibly inhibits the activity of carnitine palmitoyltransferase I. As a result, fatty acid import into the mitochondria and β-oxidation is reduced, whereas cytosolic fatty acid accumulates and glucose oxidation is elevated. Prolonged incubation (24 h) with Etomoxir produces diverse effects on the expression of several metabolic enzyme[2].

    In Vivo

    Etomoxir is an inhibitor of free fatty acid (FFA) oxidation-related key enzyme CPT1. P53 interacts directly with Bax, which is inhibited by Etomoxir, further confirming the direct interaction of P53 and Bax, and the involvement of FAO-mediated mitochondrial ROS generation in db/db mice[3]. Rats are injected daily with Etomoxir, a specific CPT-I inhibitor, for 8 days at 20 mg/kg of body mass. Etomoxir-treated rats display a 44% reduced cardiac CPT-I activity. The treatment of Lewis rats for 8 days with 20 mg/kg Etomoxir does not alter blood glucose, which is in line with comparable etomoxir-feeding studies. Similarly, Etomoxir feeding does not affect general growth characteristics such as gain in body mass, nor does it affect hindlimb muscle mass. However, heart mass and liver mass are both significantly increased by 11% in Etomoxir-treated rats[4].

    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 3.0598 mL 15.2989 mL 30.5979 mL
    5 mM 0.6120 mL 3.0598 mL 6.1196 mL
    10 mM 0.3060 mL 1.5299 mL 3.0598 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay

    Etomoxir is dissolved in DMSO and stored, and then diluted with appropriate medium before use[2].

    Rat heart H9c2 myoblastic cells are incubated in DMEM containing 10% fetal bovine serum until near confluence. In some experiments, cells are preincubated for 2 h with DMEM (serum-free) in the absence or presence of 1-80 μM Etomoxir and then incubated for 2 h with 0.1 mM [1-14C]oleic acid (10 μCi/dish, binds to BSA in a 1:1 molar ratio). In other experiments, cells are preincubated for 2 h plus or minus 40 μM Etomoxir and then incubated for 2 h with 0.1 μM or 0.1 mM [1,3-3H]glycerol (10 μCi/dish), 0.1 mM [1-14C]oleic acid (2 μCi/dish, binds to BSA in a 1:1 molar ratio), 0.1 mM [1-14C]palmitic acid (2 μCi/dish, binds to BSA in a 1:1 molar ratio), 28 μM [3H]ethanolamine (2 μCi/dish), 28 μM [methyl-3H]choline (2 μCi/dish), 0.4 mM [3H]serine (20 μCi/dish), or 40 μM myo-[3H]inositol (10 μCi/dish). The medium is removed and the cells washed twice with ice-cold saline and then harvested from the dish with 2 mL methanol-water (1:1, v/v) for lipid extraction. An aliquot of the homogenate is taken for the determination of total uptake of radioactivity into cells. Phospholipids are then isolated and radioactivity in these determined[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration

    Etomoxir is dissolved in 0.9% (w/v) NaCl (rats)[4].

    80 male C57BLKS/J lar-Leprdb/db mice and 20 wild type littermates (8 week) are used. db/db mice are randomly divided into four groups: db/db group, Etomoxir group, MitoQ group, and PFT-α group. In the Etomoxir group, mice are intraperitoneally injected with 1 mg/kg Etomoxir twice every week. In the MitoQ group, 50 μM MitoQ is given to the mice in water. Water bottles, containing either MitoQ, are covered with aluminum foil, and all bottles are refilled every 3 days. In the PFT-α group, mice are intraperitoneally injected with 1 mg/kg PFT-α twice every week. WT mice are administrated with vehicle instead. The experimental period is 8 weeks. At the end, peripheral blood samples and bone marrow cells are harvested for the assays.
    Male Lewis rats, weighing 150-200 g, are used in the present study. Animals are kept on a 12 h:12 h light/dark cycle and fed a Purina Chow diet and water ad libitum. The rats are divided into two groups: (1) control and (2) Etomoxir. Etomoxir (20 mg/kg of body weight) is dissolved in 0.9% (w/v) NaCl and administered intraperitoneally for 8 days. Control rats receive saline. The last injection is given 24 h before the experiment. Animals are anaesthetized with an intraperitoneal injection of a nembutal and heparin (3:1) mixture. Subsequently, the heart is removed for LCFA uptake studies and for analyses of transporter protein contents. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight




    CAS No.



    O=C(OCC)[[email protected]@]1(OC1)CCCCCCOC2=CC=C(C=C2)Cl


    4°C, protect from light, stored under nitrogen


    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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