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Etomoxir((R)-(+)-Etomoxir) sodium salt 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 is developed as an inhibitor of the mitochondrial carnitine palmitoyltransferase-1 (CPT-1) located on the outer mitochondrial membrane. (R)-(+)-Etomoxir sodium salt is R-form of Etomoxir sodium salt. Etomoxir, in the liver can act as peroxisomal proliferator, increasing DNA synthesis and liver growth. Etomoxir is an inhibitor of free fatty acid (FFA) oxidation-related key enzyme CPT1. Etomoxir has also been identified as a direct agonist of PPARα.
Etomoxir significantly inhibits the decrease of bone mineral density (BMD) and bone breaking strength in db/db and high fat (HF)-fed mice and suppresses the reduction of BMSCs-differentiated osteoblasts. Etomoxir inhibits the increase of mitochondrial ROS generation in db/db and HF-fed mice and osteoblasts.
J Hepatol. 2022 Nov 9;S0168-8278(22)03285-8.
Hepatocyte-specific Mas activation enhances lipophagy and fatty acid oxidation to protect against acetaminophen-induced hepatotoxicity in mice
Etomoxir sodium salt purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | Pulmonary artery smooth muscle cells |
| Preparation method | The proliferation of vascular smooth muscle cells was induced by 10–30 ng/mL PDGF-BB. It was shown that the proliferation of PASMCs was also stimulated by PDGF-BB at the similar concentration. After digestion, PASMCs were digested and were cultured in DMEM with 15% FBS. When the cells tended to 80–90% confluences, the medium was replaced by DMEM with 0.02% FBS and starved for 24 h. The cells were pretreated with different doses of ETO (3, 10, 30, 100 µM ETO) for 1 h, and then treated with PDGF-BB (10–30 ng/mL). After incubation for indicated times, PAMSCs were collected and tested. |
| Concentrations | 3, 10, 30, 100, and 300 µM |
| Incubation time | 1 h |
| Animal Experiment | |
|---|---|
| Animal models | male C57BLKS/J lar-Leprdb/db mice |
| Formulation | Saline |
| Dosages | 1 mg/kg twice every week |
| Administration | intraperitoneally injected |
| Molecular Weight | 320.74 |
| Formula | C15H18ClNaO4 |
| CAS Number | 828934-41-4 |
| Form | Solid |
| Solubility (25°C) | DMSO 45 mg/mL Water 5 mg/mL |
| Storage | -20°C, protect from light, sealed |
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