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. Lovastatin is an HMG-CoA reductase inhibitor that was initially isolated from Aspergillus terreus. Marketed as MevinolinTM, MevacorTM, and under several other trade names, Lovastatin was the first HMG-CoA reductase inhibitor to be used in the treatment of hypercholesterolemia. It is a competitive inhibitor of HMG-CoA reductase with a Ki value of 0.6 nM for the open ring, hydroxy acid form of the molecule. During a three week study in dogs, a dose of 8 mg/kg per day resulted in a 29% reduction in plasma cholesterol. Lovastatin also suppresses TNF-induced NF-.kappa.B activation -IC50 ~ 15 uM), which potentiates apoptosis in human myeloid leukemia cells and thus, maybe useful in treating cancer.
產(chǎn)品描述
A potent, competitive inhibitor of HMG-CoA reductase -Ki = 0.6 nM)