Hydroxymethylglutaryl-coenzyme A -HMG-CoA) reductase is the rate-limiting enzyme in the cholesterol biosynthetic pathway and the target of the statin class of cholesterol-lowering drugs. Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki value of 0.12 nM for the hydrolyzed, open ring form of the molecule. Simvastatin is marketed under the trade name ZocorTM and is often prescribed in combination with ezetimibe -Zetia) to treat dyslipidemia. This drug combination is known commercially as VytorinTM or InegyTM. After 18 days of treatment with simvastatin in dogs at a dose of 8 mg/kg per day, plasma cholesterol levels were reduced by 33%. Simvastatin also suppresses TNF-induced NF-.kappa.B activation -IC50 ~ 13 uM), which potentiates apoptosis in human myeloid leukemia cells and thus may be useful in treating cancer.
產(chǎn)品描述
A potent, competitive inhibitor of HMG-CoA reductase -Ki = 0.12 nM)