Etomoxir sodium salt

製品コードS8244 バッチS824403

印刷

化学情報

Chemical Structure 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 64 mg/mL warmed with 50ºC water bath (199.53 mM)
Ethanol 8 mg/mL (24.94 mM)
* <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 has also been identified as a direct agonist of PPARα. Etomoxir is a compound that 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]. Etomoxir 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 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. Etomoxir 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 etomoxir 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, etomoxir has a selective influence on the rate of contraction and relaxation of overloaded hearts. Etomoxir, 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. Etomoxir reduces inflammation and demyelination in the CNS of treated mice[2]. Inhibition of fatty acid oxidation by etomoxir 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. Etomoxir 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 MOG35-55 peptide s.c., and 14 days later splenocytes are isolated and cultured at a concentration of 6×106 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 etomoxir. 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.

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：

Extracellular matrix stiffness as an energy metabolism regulator drives osteogenic differentiation in mesenchymal stem cells [ Bioact Mater, 2024, 35:549-563] PubMed: 38434800
PIM1 drives lipid droplet accumulation to promote proliferation and survival in prostate cancer [ Oncogene, 2024, 43(6):406-419] PubMed: 38097734
Targeting metabolic adaptive responses induced by glucose starvation inhibits cell proliferation and enhances cell death in osimertinib-resistant non-small cell lung cancer (NSCLC) cell lines [ Biochem Pharmacol, 2024, S0006-2952(24)00144-8] PubMed: 38522556
NINJ1 regulates ferroptosis via xCT antiporter interaction and CoA modulation [ bioRxiv, 2024, 2024.02.22.581432] PubMed: 38464226
Immuno-metabolic dendritic cell vaccine signatures associate with overall survival in vaccinated melanoma patients [ Nat Commun, 2023, 10.1038/s41467-023-42881-4] PubMed: 37938561
Restoration of CPT1A-mediated fatty acid oxidation in mesothelial cells protects against peritoneal fibrosis [ Theranostics, 2023, 13(13):4482-4496] PubMed: 37649600
Restoration of CPT1A-mediated fatty acid oxidation in mesothelial cells protects against peritoneal fibrosis [ Theranostics, 2023, 10.7150/thno.84921] PubMed: 37649600
Perturbation of Copper Homeostasis Sensitizes Cancer Cells to Elevated Temperature [ Int J Mol Sci, 2023, 25(1)423] PubMed: 38203594
Metabolomic analysis of pig spleen reveals African swine fever virus infection increased acylcarnitine levels to facilitate viral replication [ J Virol, 2023, 97(8):e0058623] PubMed: 37582206
Metabolomic analysis of pig spleen reveals African swine fever virus infection increased acylcarnitine levels to facilitate viral replication [ J Virol, 2023, 97(8):e0058623] PubMed: 37582206

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。