2. Apoptosis
  3. Apoptosis
  4. Etomoxir

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

Cat. No.: HY-50202 Purity: 99.92%
COA Handling Instructions

Etomoxir ((R)-(+)-Etomoxir) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.

For research use only. We do not sell to patients.

Etomoxir Chemical Structure

Etomoxir Chemical Structure

CAS No. : 124083-20-1

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Customer Review

Based on 59 publication(s) in Google Scholar

Other Forms of Etomoxir:

Etomoxir Related Antibodies

Top Publications Citing Use of Products

57 Publications Citing Use of MCE Etomoxir

WB
Proliferation Assay

    Etomoxir purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Feb 15;14(2):125.  [Abstract]

    Etomoxir reduces the proliferation of 143b cells.

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

    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.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Etomoxir ((R)-(+)-Etomoxir) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.

    IC50 & Target

    CPT-1a[5]
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Etomoxir Related Antibodies
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    326.82

    Appearance

    <32°C Solid,>34°C Liquid

    Formula

    C17H23ClO4
    CAS No.
    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage

    -20°C, protect from light, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (305.98 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent 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.
    In Vivo:
    • 1.

      Add each solvent one by one:  0.5% Methylcellulose/saline water

      Solubility: 10 mg/mL (30.60 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 3.5 mg/mL (10.71 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 3.5 mg/mL (10.71 mM); Clear solution

    • 4.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.5 mg/mL (7.65 mM); Clear solution; Need ultrasonic

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.92%

    COA (242 KB) RP-HPLC (184 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [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 [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
    [3][4]

    Mice[3]
    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.
    Rats[4]
    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
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    Etomoxir Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    Etomoxir124083-20-1(R)-(+)-EtomoxirApoptosisInhibitorinhibitorinhibit

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