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> Etomoxir (sodium salt) [828934-41-4]

Etomoxir (sodium salt) [828934-41-4]

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Katalog-Nummer HY-50202A-50mg

Size : 50mg

Marke : MedChemExpress


Beschreibung

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

 

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.
Molekulargewicht

320.74

Formel

C15H18ClNaO4
CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=C(OCCCCCC[C@@]2(CO2)C(O[Na])=O)C=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

*In solvent : -80°C, 2 years; -20°C, 1 year (protect from light, stored under nitrogen)

Lösungsmittel & Löslichkeit
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
Concentration Solvent Mass 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
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.

Select the appropriate dissolution method based on your experimental animal and administration route.

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 μL DMSO 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 μL DMSO 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.

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
Reinheit & Dokumentation
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