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Etomoxir Sale

(Synonyms: 乙莫克舍,R-(+)-Etomoxir,Etomoxir) 目录号 : GC16736

Etomoxir ((R)-(+)-Etomoxir) 是肉碱棕榈酰转移酶 1a (CPT-1a) 的不可逆抑制剂,通过 CPT-1a 抑制脂肪酸氧化 (FAO) 并抑制人、大鼠中的棕榈酸酯 β-氧化和豚鼠。

Etomoxir Chemical Structure

Cas No.:124083-20-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥616.00
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5mg
¥560.00
现货
10mg
¥1,050.00
现货
50mg
¥3,710.00
现货
100mg
¥5,670.00
现货

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Sample solution is provided at 25 µL, 10mM.

客户使用产品发表文献 3

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Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

Rat heart H9c2 myoblastic cells

Preparation method

This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1-80 μM; 2 h

Applications

In rat heart H9c2 myoblastic cells, Etomoxir concentration-dependently reduced [1-14C]oleic acid incorporation into phosphatidylglycerol (PtdGro) and cardiolipin (CL). In contrast, etomoxir increased [1,3-3H]glycerol incorporation into CL.

Animal experiment [2]:

Animal models

Experimental autoimmune encephalomyelitis (EAE) mice model

Dosage form

15 mg/kg i.p.; days 8 and 15

Application

In experimental autoimmune encephalomyelitis (EAE) mice, Etomoxir reduced disease severity and the inflammatory response. Etomoxir-treated mice displayed a reduced immune cell infiltration in the CNS with few macrophages, activated microglia, or T cells present. Etomoxir also reduced inflammation and demyelination in the CNS.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Xu FY1, Taylor WA, Hurd JA, 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.

[2] Shriver LP1, Manchester M. Inhibition of fatty acid metabolism ameliorates disease activity in an animal model of multiple sclerosis. Sci Rep. 2011;1:79.

产品描述

Etomoxir ((R)-(+)-Etomoxir) 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.

Etomoxir binds irreversibly to the catalytic site of CPT-1 inhibiting its activity, but also upregulates fatty acid oxidation enzymes. Etomoxir is developed as an inhibitor of the mitochondrial carnitine palmitoyltransferase-1 (CPT-1) located on the outer mitochondrial membrane. Etomoxir, in the liver can act as peroxisomal proliferator, increasing DNA synthesis and liver growth. Thus, etomoxir, in addition of being a CPT1 inhibitor could be considered as a PPARalpha agonist[1]. Etomoxir is a member of the oxirane carboxylic acid carnitine palmitoyl transferase I inhibitors and has been suggested as a therapeutic agent for the treatment of heart failure. Acute Etomoxir treatment irreversibly inhibits the activity of carnitine palmitoyltransferase I. As a result, fatty acid import into the mitochondria and β-oxidation is reduced, whereas cytosolic fatty acid accumulates and glucose oxidation is elevated. Prolonged incubation (24 h) with Etomoxir produces diverse effects on the expression of several metabolic enzyme[2].

Etomoxir is an inhibitor of free fatty acid (FFA) oxidation-related key enzyme CPT1. P53 interacts directly with Bax, which is inhibited by Etomoxir, further confirming the direct interaction of P53 and Bax, and the involvement of FAO-mediated mitochondrial ROS generation in db/db mice[3]. Rats are injected daily with Etomoxir, a specific CPT-I inhibitor, for 8 days at 20 mg/kg of body mass. Etomoxir-treated rats display a 44% reduced cardiac CPT-I activity. The treatment of Lewis rats for 8 days with 20 mg/kg Etomoxir does not alter blood glucose, which is in line with comparable etomoxir-feeding studies. Similarly, Etomoxir feeding does not affect general growth characteristics such as gain in body mass, nor does it affect hindlimb muscle mass. However, heart mass and liver mass are both significantly increased by 11% in Etomoxir-treated rats[4].

References:
[1]. Rupp H, et al. The use of partial fatty acid oxidation inhibitors for metabolic therapy of angina pectoris and heart failure. Herz. 2002 Nov;27(7):621-36.
[2]. Xu FY, 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.
[3]. Li J, 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.
[4]. Luiken JJ, et al. Etomoxir-induced partial carnitine palmitoyltransferase-I (CPT-I) inhibition in vivo does not alter cardiac long-chain fatty acid uptake and oxidation rates. Biochem J. 2009 Apr 15;419(2):447-55.
[5]. O'Connor RS, et al. The CPT1a inhibitor, etomoxir induces severe oxidative stress at commonly used concentrations. Sci Rep. 2018 Apr 19;8(1):6289.

Chemical Properties

Cas No. 124083-20-1 SDF
别名 乙莫克舍,R-(+)-Etomoxir,Etomoxir
化学名 ethyl (2R)-2-[6-(4-chlorophenoxy)hexyl]oxirane-2-carboxylate
Canonical SMILES CCOC(=O)C1(CO1)CCCCCCOC2=CC=C(C=C2)Cl
分子式 C17H23ClO4 分子量 326.82
溶解度 ≥ 32.7 mg/mL in DMSO, ≥ 109.6 mg/mL in EtOH, ≥ 48.3 mg/mL in Water with gentle warming 储存条件 Store at -20°C, protect from light, stored under nitrogen
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 3.0598 mL 15.2989 mL 30.5979 mL
5 mM 0.612 mL 3.0598 mL 6.1196 mL
10 mM 0.306 mL 1.5299 mL 3.0598 mL
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