Etomoxir sodium salt

製品コードS8244 バッチS824407

印刷

化学情報

Synonyms

(R)-(+)-Etomoxir sodium salt

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₅H₁₈ClO₄.Na

分子量

320.74

CAS No.

828934-41-4

Solubility (25°C)*

体外

DMSO

64 mg/mL (199.53 mM)

Water (warmed with 50ºC water bath)

64 mg/mL (199.53 mM)

Ethanol

11 mg/mL (34.29 mM)

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	3.200mg/ml (9.98mM)	Taking the 1 mL working solution as an example, add 50 μL 64 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase-1 (CPT-1) on the outer face of the inner mitochondrial membrane. Etomoxir enhances palmitate-induced cell apoptosis.
in vitro	Etomoxir sodium salt has also been identified as a direct agonist of PPARα. This compound binds irreversibly to the catalytic site of CPT-1 inhibiting its activity, but also upregulates fatty acid oxidation enzymes. Transcriptional effects of etomoxir could be due to 1. shift in energy metabolism with increased glucose utilization and 2. PPARalpha activation^[1]. It reduces pro-inflammatory cyokine production and increases apoptosis of MOG specific T cells^[2]. Etomoxir has been shown to decrease oxygen consumption rates (OCRs) and impair ATP and NADPH production in the pediatric glioblastoma cell line SF188^[3].
in vivo	Etomoxir sodium salt has a protective action on the ischemia/reperfusion injury of the kidney similarly to an established PPARalpha agonist. It has been developed for treating non-insulindependent diabetes mellitus. This compound increases the functional recovery of fatty acid perfused ischemic rat hearts which is unrelated to changes in levels of long-chain acylcarnitines and is attributed to an increased glucose use. A chronic treatment of rats with this chemical increases the SR Ca2+-ATPase activity, the Ca2+ uptake rate, the number of active Ca2+ pumps E~P, the SERCA2 protein and the SERCA2 mRNA abundance of the heart. At a low dosage, it has a selective influence on the rate of contraction and relaxation of overloaded hearts. This compound, in the liver can act as peroxisomal proliferator, increasing DNA synthesis and liver growth^[1]. Etomoxir-treated mice displays a reduced immune cell infiltration in the CNS with few macrophages, activated microglia, or T cells present. It reduces inflammation and demyelination in the CNS of treated mice^[2]. Inhibition of fatty acid oxidation by this chemical prolongs survival time in a syngeneic mouse model of malignant glioma and slow tumor growth. Emergence and progression of glioma are delayed upon treatment with the investigational drug etomoxir. It has already been tested in phase I/II clinical trials for treating moderate congestive heart failure; this trial is discontinued because 4 patients (of 226 taking the drug) developed unacceptably high liver transaminase levels upon treatment, and the risk of such drastic side effects is deemed sufficient to negate the potential benefit of this drug for these patients^[3].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Splenocytes
	濃度	100 μM
	反応時間	72 h
	実験の流れ	C57BL/6 mice are immunized with 200 μg MOG_35-55 peptide s.c., and 14 days later splenocytes are isolated and cultured at a concentration of 6×10_⁶ cells/ml in DMEM containing high (4.5 g/L) or low (1 g/L) glucose, 10% FBS 50 μg/ml MOG peptide, and 25 ng/ml IL-12 (R&D systems, Minneapolis, MN) in the presence of vehicle or 100 μM this compound. 72 hours later cells are harvested for APO-BrdU staining and supernatants collected for IL-4, IL-17 and IFN-γ ELISA. (MOG:myelin oligodendrocyte glycoprotein)
動物実験	動物モデル	C57BL6/J mice
	投薬量	15 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/12439634/
https://pubmed.ncbi.nlm.nih.gov/22355598/
https://pubmed.ncbi.nlm.nih.gov/27365097/

カスタマーフィードバック

: Data from [Data independently produced by , , Cancer Lett, 2018, 442:40-52]

: Data from [Data independently produced by , , Med Sci Monit, 2018, 24:1484-1492]

: Data from [Data independently produced by , , Med Sci Monit, 2018, 24: 1484-1492]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Coenzyme A protects against ferroptosis via CoAlation of mitochondrial thioredoxin reductase [ J Clin Invest, 2025, e190215]	PubMed: 40694424
Inhibition of adenosine/A2A receptor signaling suppresses dermal fibrosis by enhancing fatty acid oxidation [ Cell Commun Signal, 2025, 23(1):206]	PubMed: 40301970
Autophagic flux-lipid droplet biogenesis cascade sustains mitochondrial fitness in colorectal cancer cells adapted to acidosis [ Cell Death Discov, 2025, 11(1):21]	PubMed: 39856069
Comprehensive characterization of fatty acid oxidation in triple-negative breast cancer: Focus on biological roles and drug modulation [ Eur J Pharmacol, 2025, 991:177343]	PubMed: 39900330
Metabolic imprinting drives epithelial memory during mucosal fungal infection [ bioRxiv, 2025, 2025.07.11.664387]	PubMed: 40791350
Extracellular matrix stiffness as an energy metabolism regulator drives osteogenic differentiation in mesenchymal stem cells [ Bioact Mater, 2024, 35:549-563]	PubMed: 38434800
NINJ1 regulates ferroptosis via xCT antiporter interaction and CoA modulation [ Cell Death Dis, 2024, 15(10):755]	PubMed: 39424803
Small molecules targeting selective PCK1 and PGC-1α lysine acetylation cause anti-diabetic action through increased lactate oxidation [ Cell Chem Biol, 2024, 31(10):1772-1786.e5]	PubMed: 39341205
PIM1 drives lipid droplet accumulation to promote proliferation and survival in prostate cancer [ Oncogene, 2024, 43(6):406-419]	PubMed: 38097734
Monocyte and macrophage profiles in patients with inherited long-chain fatty acid oxidation disorders [ Biochim Biophys Acta Mol Basis Dis, 2024, 1871(1):167524]	PubMed: 39307292

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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