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Etomoxir sodium salt

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Chemical Structure| 828934-41-4 同义名 : (R)-(+)-Etomoxir Sodium;(+)-Etomoxir (sodium salt);(R)-(+)-Etomoxir;(R)-(+)-Etomoxir sodium salt
CAS号 : 828934-41-4
货号 : A108121
分子式 : C15H18ClNaO4
纯度 : 99%+
分子量 : 320.744
MDL号 : MFCD07787411
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(155.89 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 5 mg/mL(15.59 mM)，配合低频超声助溶
动物实验配方：

PO 0.5% CMC-Na 30 mg/mL suspension

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[3]. (R)-(+)-etomoxir sodium salt 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[4]. 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[3]. 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[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.12mL

0.62mL

0.31mL

15.59mL

3.12mL

1.56mL

31.18mL

6.24mL

3.12mL
参考文献

[1]Yao CH, Liu GY, Wang R, Moon SH, Gross RW, Patti GJ. Identifying off-target effects of etomoxir reveals that carnitine palmitoyltransferase I is essential for cancer cell proliferation independent of β-oxidation. PLoS Biol. 2018 Mar 29;16(3):e2003782. doi: 10.1371/journal.pbio.2003782. PMID: 29596410; PMCID: PMC5892939.

[2]Lopaschuk GD, Wall SR, Olley PM, Davies NJ. Etomoxir, a carnitine palmitoyltransferase I inhibitor, protects hearts from fatty acid-induced ischemic injury independent of changes in long chain acylcarnitine. Circ Res. 1988 Dec;63(6):1036-43. doi: 10.1161/01.res.63.6.1036. PMID: 3197271.

[3]Ratheiser K, Schneeweiss B, Waldhäusl W, Fasching P, Korn A, Nowotny P, Rohac M, Wolf HP. Inhibition by etomoxir of carnitine palmitoyltransferase I reduces hepatic glucose production and plasma lipids in non-insulin-dependent diabetes mellitus. Metabolism. 1991 Nov;40(11):1185-90. doi: 10.1016/0026-0495(91)90214-h. PMID: 1943747.