HMG-CoA reductase inhibitor. Cholesterol lowering drug. Inhibits myoblast formation. An antibiotic shown to cause apoptosis, apparently by inhibiting post-translational prenylation of proteins such as Ras. Similarly, mevastatin increases eNOS mRNA and protein levels by blocking the geranylgeranylation of Rho.
Lovastatin is a cholesterol lowering drug and competitive inhibitor of HMG-CoA reductase, a rate limiting enzyme in cholesterol synthesis. Blocks the production of mevalonate, a critical compound in the production of cholesterol and isoprenoids. This product is a substrate of Pgp and CYP3A. It increases cellular resistance to anticancer agents such as doxorubicin and induces apoptosis in myeloma cells. The roles of Pgp and CYP3A, possible connection between drug resistance, regulation of the mevalonate pathway, and iosprenylation of signaling proteins in these observations remain to be resolved. The product induces apoptosis in numerous cancer cell lines perhaps, in part, by inhibiting the isoprenylation of Rho family GTPases. It causes cell cycle arrest in G1 and G2/M phases.
Simvastatin is a specific inhibitor of HMG-CoA reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonate, an early step in cholesterol biosynthesis. It is used in the treatment of hypercholesterolemia, as it reduces levels of low-density lipoproteins and triglycerides, and raises high-density lipoprotein levels. Simvastatin is a lactone that is readily hydrolyzed in vivo to the corresponding β-hydroxyacid, and can be activated prior to use with NaOH in EtOH treatment. It is a synthetic analog of lovastatin (Cat. No. M2147). Simvastatin, a synthetic analog of lovastatin, is a specific inhibitor of HMG-CoA reductase (3-hydroxy-3-methyl-glutaryl-CoA reductase.) HMG-CoA is a major therapeutic target for reduction of low density lipoprotein (LDL) cholesterol. Simvastatin may also have beneficial effects on endothelial function, smooth muscle cell function, hemostasis, vascular wall function, LDL oxidation, and inflammation. Simvastatin can be activated prior to use by treatment with NaOH in EtOH.
SR 12813 is a pregnane X receptor (PXR, NR 112) agonist; cholesterol lowering drug; HMGCoA reductase inhibitor. SR-12813 is a 1,1-bisphosphonate ester that exhibits hypocholesterolemic activity.1 It decreases the biosynthesis of cholesterol by enhancing the degradation of HMG-CoA reductase.2