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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Etomoxir sodium salt Chemical Structure
CAS No. : 828934-41-4
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Based on 82 publication(s) in Google Scholar
Other Forms of Etomoxir sodium salt:
Etomoxir
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(S)-(+)-Etomoxir
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Etomoxir sodium salt purchased from MedChemExpress. Usage Cited in:
Cell Death Dis. 2023 Feb 15;14(2):125.
[Abstract]
Etomoxir reduces the proliferation of 143b cells.
Etomoxir sodium salt 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.
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Description
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[1].
IC50 & Target
CPT-1a[2]
In Vitro
Etomoxir mediates differential metabolic channeling of fatty acid and glycerol precursors into cardiolipin in H9c2 cells[2].
Etomoxir does not affect the activities of the cardiolipin biosynthetic and remodeling enzymes but causes a reduction in [1-14C]palmitic acid or [1-14C]oleic acid incorporation into cardiolipin[2].
Etomoxir increases [1,3-3H]glycerol incorporation into cardiolipin. The mechanism is a 33% increase in glycerol kinase activity, which produces an increased glycerol flux through the de novo pathway of cardiolipin biosynthesis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Etomoxir sodium salt Related Antibodies
Cell Viability Assay[2]
Cell Line:
Rat heart H9c2 myoblastic cells
Concentration:
1-80 μM
Incubation Time:
2 hours
Result:
Reduced the incorporation of [1-14C]fatty acids into CL and PtdGro in H9c2 cardiac myoblast cells but did not affect total incorporation of radioactivity into these cells.
In Vivo
Etomoxir 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[3].
Etomoxir inhibits the increase of mitochondrial ROS generation in db/db and HF-fed mice and osteoblasts[3].
Etomoxir-induced partial carnitine palmitoyltransferase-I (CPT-I) inhibition in vivo does not alter cardiac long-chain fatty acid uptake and oxidation rates[4]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
80 male C57BLKS/J lar-Leprdb/db mice[3]
Dosage:
1 mg/kg
Administration:
Intraperitoneally injected; twice every week
Result:
Serum alkaline phosphatase was increased in db/db mice, which event was significantly suppressed by Etomoxir.
Serum level of osteocalcin, a marker of bone formation, was reduced in db/db mice and Etomoxir markedly inhibited the reduction of osteocalcin.
Serum tartrate-resistant acid phosphatase was elevated in db/db mice which phenomenon was significantly suppressed by Etomoxir.
Animal Model:
Rats[4]
Dosage:
20 mg/kg
Administration:
Injected daily; for 8 days
Result:
Etomoxir-treated rats displayed a 44% reduced cardiac CPT-I activity.
Molecular Weight
320.74
Formula
C15H18ClNaO4
CAS No.
828934-41-4
Appearance
Solid
Color
White to off-white
SMILES
ClC1=CC=C(OCCCCCC[C@@]2(CO2)C(O[Na])=O)C=C1
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, protect from light, stored under nitrogen
*In solvent : -80°C, 2 years; -20°C, 1 year (protect from light, stored under nitrogen)
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (155.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 5 mg/mL (15.59 mM; Need ultrasonic)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
3.1178 mL
15.5890 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
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light, stored under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (7.79 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.79 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3
Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.79 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μLCorn oil, and mix evenly.
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution.
If precipitation or phase separation occurs during preparation,
heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: PBS
Solubility: 3.33 mg/mL (10.38 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
*In solvent : -80°C, 2 years; -20°C, 1 year (protect from light, stored under nitrogen)
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
[1]. Roddy S O'Connor, et al. The CPT1a inhibitor, etomoxir induces severe oxidative stress at commonly used concentrations.Sci Rep. 2018 Apr 19;8(1):6289.
[Content Brief]
[2]. Fred Y Xu,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.
[Content Brief]
[3]. Jun Li, 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.
[Content Brief]
[4]. Joost J F P Luiken, et al. Etomoxir-induced partial carnitine palmitoyltransferase-I (CPT-I) inhibition in vivo does not alter cardiac long-chain fatty acid uptake and oxidation rates.Biochem J. 2009 Apr 15;419(2):447-55.
[Content Brief]
[1]. Roddy S O'Connor, et al. The CPT1a inhibitor, etomoxir induces severe oxidative stress at commonly used concentrations.Sci Rep. 2018 Apr 19;8(1):6289.
[2]. Fred Y Xu,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.
[3]. Jun Li, 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.
[4]. Joost J F P Luiken, et al. Etomoxir-induced partial carnitine palmitoyltransferase-I (CPT-I) inhibition in vivo does not alter cardiac long-chain fatty acid uptake and oxidation rates.Biochem J. 2009 Apr 15;419(2):447-55.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light, stored under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
H2O / DMSO
1 mM
3.1178 mL
15.5890 mL
31.1779 mL
77.9448 mL
5 mM
0.6236 mL
3.1178 mL
6.2356 mL
15.5890 mL
10 mM
0.3118 mL
1.5589 mL
3.1178 mL
7.7945 mL
15 mM
0.2079 mL
1.0393 mL
2.0785 mL
5.1963 mL
DMSO
20 mM
0.1559 mL
0.7794 mL
1.5589 mL
3.8972 mL
25 mM
0.1247 mL
0.6236 mL
1.2471 mL
3.1178 mL
30 mM
0.1039 mL
0.5196 mL
1.0393 mL
2.5982 mL
40 mM
0.0779 mL
0.3897 mL
0.7794 mL
1.9486 mL
50 mM
0.0624 mL
0.3118 mL
0.6236 mL
1.5589 mL
60 mM
0.0520 mL
0.2598 mL
0.5196 mL
1.2991 mL
80 mM
0.0390 mL
0.1949 mL
0.3897 mL
0.9743 mL
100 mM
0.0312 mL
0.1559 mL
0.3118 mL
0.7794 mL
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
Etomoxir sodium salt Related Classifications
Apoptosis
Apoptosis
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.