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CAS No.: 124083-20-1

Etomoxir/乙莫克舍 Catalog No. CSN17613

Synonyms: (R)-(+)-Etomoxir;B 807-54

Etomoxir is a cell-permeable, irreversible, and stereospecific inhibitor of carnitine palmitoyltransferase (CPT)-1 and DGAT activity in the mitochondria of rat heart H9c2 myoblastic cells at a concentration of 1-80 μM and 40 μM, respectively.

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技术信息

生物活性

描述Oxidation of long-chain fatty acids inside of the mitochondrial matrix provides an essential source of energy for some cells. Since long-chain fatty acids cannot freely pass into the mitochondrial matrix, they rely on a protein called carnitine palmitoyltransferase I (CPT1) for transport. CPT1 has been identified as a potential therapeutic target for a growing list of cancers that include breast cancer, prostate cancer, glioblastoma, colon cancer, gastric cancer, myeloma, and others. Etomoxir is an inhibitor of carnitine palmitoyltransferase I (CPT1). Etomoxir at 10^-6 M prevented the palmitate-induced depression of function in heart but did not decrease myocardial long chain acylcarnitine or long chain acyl-CoA levels, and oxygen consumption per unit work was decreased during reperfusion recovery, and ATP and creatine-phosphate levels were significantly higher after reperfusion. 200 μM of etomoxir caused a significant reduction in cellular proliferation rate in BT549 cells, while 10 μM did not. 200 μM etomoxir treatment, however, significantly impaired mitochondrial respiration in BT549 cells, and a 65% decrease in basal respiration and a 65% decrease in maximal respiratory capacity after treating cells with 200 μM etomoxir was measured. Non-insulin-dependent diabetes mellitus (NIDDM) patients who received oral etomoxir treatment twice daily at the dose of 25 mg to 100 mg showed dose-dependent decrease in fasting blood glucose.
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03144128	Cancer Cachexia ... more >> Vitamin D Deficiency Collapse <<	Not Applicable	Recruiting	December 2021	United States, Kentucky ... more >> Markey Cancer Center Recruiting Lexington, Kentucky, United States, 40536 Contact: Elizabeth Rush Collapse <<

参考文献

[1] 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.
[2] Xu FY, Taylor WA, 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. Epub 2002 Nov 4.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0598 mL
- 15.2992 mL
- 30.5983 mL
- 5 mM
- 0.6120 mL
- 3.0598 mL
- 6.1197 mL
- 10 mM
- 0.3060 mL
- 1.5299 mL
- 3.0598 mL

技术信息

CAS号

124083-20-1

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H23ClO4

运输

蓝冰

分子量

326.82

别名

(R)-(+)-Etomoxir;B 807-54

溶解度

DMSO	210.0 mg/mL (642.6 mM)
Water	insoluble

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