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

Catalog No.GC15104

Etomoxir((R)-(+)-Etomoxir) sodium salt 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.

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(R)-(+)-Etomoxir sodium salt Chemical Structure

Cas No.: 828934-41-4

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10mM (in 1mL DMSO)
$64.00
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10mg
$94.00
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50mg
$431.00
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500mg
$2,583.00
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1g
$4,099.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

Human T cells

Preparation Method

Activated T cells (day 3) were treated with 50 µM (R)-(+)-Etomoxir sodium salt every other day throughout logarithmic expansion.

Reaction Conditions

50 µM Etomoxir; every other day in 10days

Applications

Etomoxir reduces CD28-costimulated T cell proliferation without affecting T cell effector differentiation.

Animal experiment [2]:

Animal models

Male BALB/c nude mice (3 weeks old)

Preparation Method

Mice with approximately 3 mm tumors(T24 cells)were assigned to two groups (n=5) randomly. Etomoxir (40 mg/kg) and vehicle were injected intraperitoneally every other day for 20 days.

Dosage form

40 mg/kg;i.p; every other day for 20 days

Applications

Etomoxir suppressed human bladder cancer (BCa) cell growth in vivo.

References:

[1]. O'Connor RS, Guo L, et,al. The CPT1a inhibitor, etomoxir induces severe oxidative stress at commonly used concentrations. Sci Rep. 2018 Apr 19;8(1):6289. doi: 10.1038/s41598-018-24676-6. PMID: 29674640; PMCID: PMC5908836.
[2]. Cheng S, Wang G, et,al. Fatty acid oxidation inhibitor etomoxir suppresses tumor progression and induces cell cycle arrest via PPARγ-mediated pathway in bladder cancer. Clin Sci (Lond). 2019 Aug 7;133(15):1745-1758. doi: 10.1042/CS20190587. PMID: 31358595.

Background

(R)-(+)-Etomoxir sodium salt(Etomoxir) is a small molecule developed for metabolic and cardiovascular disease that exhibits nanomolar potency toward CPT-1a and CPT-1b upon enzymatic conversion to the active inhibitor etomoxiryl CoA (IC50 = 0.01-0.70 µM) [1-3].

Etomoxir (50 µM ETO; every other day in 10days) reduces CD28-costimulated T cell proliferation without affecting T cell effector differentiation[4]. Low concentrations(3µM,24h) of etomoxir effectively inhibit CPT-1 but do not affect M(IL-4) polarization, High concentrations of Etomoxir (200 µM) inhibit M(IL-4) polarization independently of CPT-1 activity in BMDM cells[5]. Besides the effect of etomoxil on T cell differentiation and function was independent of Cpt1a expression [6].

Etomoxir (40 mg/kg;i.p; every other day for 20 days) suppressed human bladder cancer (BCa) cell growth in vivo[7]. Etomoxir (i.p; 1 mg/kg Etomoxir; twice every week) significantly inhibits the decrease of bone mineral density (BMD) and bone breaking strength in db/db and high fat (HF)-fed mice and suppresses the reduction of BMSCs-differentiated osteoblasts [8].

References:
[1]. O'Connor RS, Guo L, et,al.The CPT1a inhibitor, etomoxir induces severe oxidative stress at commonly used concentrations. Sci Rep. 2018 Apr 19;8(1):6289. doi: 10.1038/s41598-018-24676-6. PMID: 29674640; PMCID: PMC5908836.
[2]. Divakaruni AS, Hsieh WY, et,al. Etomoxir Inhibits Macrophage Polarization by Disrupting CoA Homeostasis. Cell Metab. 2018 Sep 4;28(3):490-503.e7. doi: 10.1016/j.cmet.2018.06.001. Epub 2018 Jun 28. PMID: 30043752; PMCID: PMC6125190.
[3]. Ceccarelli SM, Chomienne O, et,al. Carnitine palmitoyltransferase (CPT) modulators: a medicinal chemistry perspective on 35 years of research. J Med Chem. 2011 May 12;54(9):3109-52. doi: 10.1021/jm100809g. Epub 2011 Apr 19. PMID: 21504156.
[4]. O'Connor RS, Guo L, et,al. The CPT1a inhibitor, etomoxir induces severe oxidative stress at commonly used concentrations. Sci Rep. 2018 Apr 19;8(1):6289. doi: 10.1038/s41598-018-24676-6. PMID: 29674640; PMCID: PMC5908836.
[5]. Divakaruni AS, Hsieh WY, et,al. Etomoxir Inhibits Macrophage Polarization by Disrupting CoA Homeostasis. Cell Metab. 2018 Sep 4;28(3):490-503.e7. doi: 10.1016/j.cmet.2018.06.001. Epub 2018 Jun 28. PMID: 30043752; PMCID: PMC6125190.
[6]. Raud B, Roy DG, et,al. Etomoxir Actions on Regulatory and Memory T Cells Are Independent of Cpt1a-Mediated Fatty Acid Oxidation. Cell Metab. 2018 Sep 4;28(3):504-515.e7. doi: 10.1016/j.cmet.2018.06.002. Epub 2018 Jun 28. PMID: 30043753; PMCID: PMC6747686.
[7]. Cheng S, Wang G, et,al.Fatty acid oxidation inhibitor etomoxir suppresses tumor progression and induces cell cycle arrest via PPARγ-mediated pathway in bladder cancer. Clin Sci (Lond). 2019 Aug 7;133(15):1745-1758. doi: 10.1042/CS20190587. PMID: 31358595.
[8]. Li J, He W, et,al.FFA-ROS-P53-mediated mitochondrial apoptosis contributes to reduction of osteoblastogenesis and bone mass in type 2 diabetes mellitus. Sci Rep. 2015 Jul 31;5:12724. doi: 10.1038/srep12724. PMID: 26226833; PMCID: PMC4521203.

Chemical Properties

Cas No. 828934-41-4 SDF
Synonyms (R)(+)Etomoxir
Chemical Name sodium (R)-2-(6-(4-chlorophenoxy)hexyl)oxirane-2-carboxylate
Canonical SMILES ClC1=CC=C(C=C1)OCCCCCC[C@@]2(C([O-])=O)OC2.[Na+]
Formula C15H18ClNaO4 M.Wt 320.74
Solubility ≥ 50mg/mL in DMSO,≥ 5mg/mL in H2O Storage Store at -20°C
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

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1 mg 5 mg 10 mg
1 mM 3.1178 mL 15.589 mL 31.1779 mL
5 mM 0.6236 mL 3.1178 mL 6.2356 mL
10 mM 0.3118 mL 1.5589 mL 3.1178 mL
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