Simvastatin 79902-63-9

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Molecular Weight:

418.57 Simvastatin is a competitive inhibitor of HMG-CoA reductase with Ki of 0.1-0.2 nM .






Biological Activity


Simvastatin inhibits cholesterol synthesis in mouse L-M cell
(fibroblast), rat H4II E cell (liver), and human Hep G2 cell (liver)
with IC50 of 19.3 nM, 13.3 nM and 15.6 nM, respectively. Simvastatin treatment leads to a dose-dependent increase in serine 473
phosphorylation of Akt within 30 minutes, with maximal phosphorylation
occurring at 1.0 µM.


Simvastatin (1.0 μM) enhances phosphorylation of
the endogenous Akt substrate endothelial nitric oxide synthase (eNOS),
inhibits serum-free media undergo Apoptosis and accelerates vascular
structure formation. Simvastatin displays
anti-inflammatory effects in vitro.


Simvastatin (10 μM) reduces
anti-CD3/anti-CD28 antibody-stimulated proliferation of PB-derived
mononuclear cells and synovial fluid cells from rheumatoid arthritis
blood, as well as IFN-γ release. Simvastatin (10 μM) suppresses
cell-mediated macrophage TNF-γ release induced via cognate interactions
by ~30%.


Simvastatin orally administration inhibits the conversion of radiolabeled acetate to cholesterol with IC50 of 0.2 mg/kg.


Simvastatin (4 mg/day) orally administration for 13 weeks to rabbits
fed an atherogenci cholesterol-rich diet, returns the
cholesterol-induced increases in total cholesterol, LDL-cholesterol and
HDL-cholesterol to normal level. Simvastatin (6 mg/kg)
produces an increase in LDL receptor-dependent binding and increases the
number of hepatic LDL receptors in rabbits fed a diet containing 0.25%
cholesterol.


Simvastatin influences inflammation
independent of its effect on plasma cholesterol level. In cynomolgus
monkeys consumed an atherogenic diet, Simvastatin (20 mg/kg/day)
induces a 1.3-fold less macrophage content in lesions, and 2-fold less
vascular cell adhesion molecule-1, interleukin-1beta, and tissue factor
expression, companied by a 2.1-fold increases in lesional smooth muscle
cell and collagen content.

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Product Categories : Metabolism > HMG-CoA Reductase Inhibitor