Clinofibrate 30299-08-2

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Molecular Weight:

468.58 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.






Biological 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.


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.

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Product Categories : Metabolism > HMG-CoA Reductase Inhibitor