product name Clinofibrate
Description: Clinofibrate inhibits hydroxymethylglutaryl coenzyme A reductase (HMGCR) with IC50 of 0.47 mM, is a lipid-lowering agent used for controlling high cholesterol and triacylglyceride levels in the blood. Clinofibrate is an antihyperlipidemic agent with IC50 with 40 μM on the activities of human liver 3α-hydroxysteroid dehydrogenases. Clinofibrate stimulates the activity of AKR 1C4 by 2.0-fold. The concentration of Clinofibrate at which maximum stimulation is achieved is 50 μM.
References: J Pharmacol Exp Ther. 1998 Jun;285(3):1096-103; Artery. 1983;12(3):145-55.
468.58
Formula
C28H36O6
CAS No.
30299-08-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 94 mg/mL (200.6 mM)
Water: <1 mg/mL
Ethanol: 94 mg/mL (200.6 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Clinofibrate is an antihyperlipidemic agent with IC50 with 40 μM on the activities of human liver 3α-hydroxysteroid dehydrogenases. Clinofibrate stimulates the activity of AKR 1C4 by 2.0-fold. The concentration of Clinofibrate at which maximum stimulation is achieved is 50 μM. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Clinofibrate significantly decreases the high plasma cholesterol level of atherosclerotic rats, which is 823 +/- 256 (mean +/- SD) mg/dl, or about ten times that of control rats (85 +/- 11 mg/dl). On treatment with Clinofibrate, the cholesterol level is reduced mostly in the very low density lipoprotein (VLDL) fraction (d less than 1.006). Heparin-releasable lipoprotein lipase activity in epididymal adipose tissue, lipoprotein lipase activity in post heparin plasma, and VLDL-triolein hydrolizing activity in adipose tissue stromal vessels are higher in Clinofibrate-treated rats than in atherosclerotic rats. Of the enzymes in the arterial wall concerned with cholesterol ester metabolism, acid cholesterol esterase activity is decreased in atherosclerotic rats, and Clinofibrate treatment increased this activity. The ratio of acyl-CoA cholesterol acyltransferase activity (ACAT) to neutral cholesterol esterase activity is higher in atherosclerotic rats than in control rats and is lower in Clinofibrate-treated rats than in atherosclerotic rats. |
| Animal model | |
| Formulation & Dosage | |
| References | J Pharmacol Exp Ther. 1998 Jun;285(3):1096-103; Artery. 1983;12(3):145-55. |
