乙莫克舍 CAS#: 124083-20-1

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乙莫克舍

生物活性靶点体外研究体内研究

中文名称	乙莫克舍
中文同义词	乙莫克舍;R-(+)-ETOMOXIR 乙莫克舍;(R)-2-(6-(4-氯苯氧基)己基)环氧乙烷-2-羧酸乙酯;依莫克舍;化合物 T4535L;ETOMOXIR乙莫克舍
英文名称	R-(+)-Etomoxir
英文同义词	(R)-2-[6-(4-Chlorophenoxy)hexyl]oxirane-2-carboxylic acid ethyl ester;2-Oxiranecarboxylic  acid,  2-[6-(4-chlorophenoxy)hexyl]-,  ethyl  ester,  (2R)-;(2S)-2-[6-(4-chlorophenoxy)hexyl]oxirane-2-carboxylic acid ethyl ester;ethyl (2S)-2-[6-(4-chlorophenoxy)hexyl]oxirane-2-carboxylate;(2R)-2-[6-(4-Chlorophenoxy)hexyl]-2-oxiranecarboxylic acid ethyl ester;2-Oxiranecarboxylic acid, 2-[6-(4-chlorophenoxy)hexyl]-, ethyl ester, (2R)-(R)-(+)-Etomoxir;S-(+)-ETOMOXIR;(S)-2-[6-(4-CHLOROPHENOXY)HEXYL]OXIRANECARBOXYLIC ACID, ETHYL ESTER
CAS号	124083-20-1
分子式	C17H23ClO4
分子量	326.82
EINECS号	200-258-5
相关类别	试剂;Chiral Reagents;Inhibitors
Mol文件	124083-20-1.mol
结构式

乙莫克舍 性质

乙莫克舍 用途与合成方法

生物活性

Etomoxir ((R)-(+)-Etomoxir) 是肉碱棕榈酰转移酶 1a (CPT-1a) 抑制剂，通过抑制 CPT-1a 可抑制脂肪酸氧化，并抑制人、大鼠和豚鼠中棕榈酸酯的氧化。

靶点

CPT-1a

体外研究

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. 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.

体内研究

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. 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.

安全信息

MSDS信息

乙莫克舍 上下游产品信息