product name Etofibrate
Description: Etofibrate is a combination of clofibrate and niacin that is used to treat hyperlipemia. Etofibrate treatment heightens the cytosolic glycerol-3-phosphate dehydrogenase activity and the total carnitine concentration in the liver of rats, whereas it reduces triacylglycerol and cholesterol concentrations. Etofibrate decreases plasma levels of cholesterol, triacylglycerols, free fatty acids (FFA) and glycerol, as well as the total and unesterified cholesterol concentrations, in liver microsomes of rats.
References: Biochim Biophys Acta. 1988 Nov 4;963(1):42-52; Biochim Biophys Acta. 1993 Jul 1;1168(3):340-7.
363.79
Formula
C18H18ClNO5
CAS No.
31637-97-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 73 mg/mL (200.7 mM)
Water: <1 mg/mL
Ethanol: 73 mg/mL (200.7 mM)
Solubility (In vivo)
Synonyms
other peoduct :
In Vitro |
In vitro activity: Etofibrate treatment heightens the cytosolic glycerol-3-phosphate dehydrogenase activity and the total carnitine concentration in the liver of rats, whereas it reduces triacylglycerol and cholesterol concentrations. Etofibrate decreases plasma levels of cholesterol, triacylglycerols, free fatty acids (FFA) and glycerol, as well as the total and unesterified cholesterol concentrations, in liver microsomes of rats. Etofibrate increases the activity of liver cytosolic glycerol-3-P dehydrogenase in the rats, whereas it decreases the activity of both microsomal HMG-CoA reductase and cholesterol 7 alpha-hydroxylase and does not affect acyl-CoA: cholesterol acyltransferase (ACAT). Etofibrate decreases the availability of lipolytic products in the liver by acting on their release from adipose tissue and on their intrinsic hepatic metabolism. Etofibrate stimulates the rate of fatty acid re-esterification when incubations are done under basal conditions in epididymal fat pad pieces from fed rats. Kinase Assay: Cell Assay: |
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In Vivo | Etofibrate (1.2 mM/g) decreases plasma FFA levels in male Sprague-Dawley rats, Etofibrate enhances or decreases plasma glycerol levels depending on both the dose and the time after treatment. Etofibrate (200 mg/kg) causes a significant inhibition of the proliferation of the smooth muscle cells in the intimal proliferate which consequently results in a less pronounced plaque in a rabbit model of atherosclerosis. |
Animal model | |
Formulation & Dosage | |
References | Biochim Biophys Acta. 1988 Nov 4;963(1):42-52; Biochim Biophys Acta. 1993 Jul 1;1168(3):340-7; Environ Toxicol Pharmacol. 1996 Dec 20;2(4):351-7. |