Lovastatin

Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol. IC50 & Target:HMG-CoA reductase^[1] In Vitro:When Lovastatin is used in cell function experiments, it is usually necessary to convert it from the inactive "lactone ring" form to the active "open-ring hydroxy acid" form^[6][7].
1. Dissolve 10 mg of Lovastatin in 0.2 mL of warm (55°C) anhydrous ethanol.
2. Add 0.1 mL of 0.6 M NaOH and 2 mL of aqueous solution and incubate at room temperature for 30 minutes.
3. Adjust the pH to 8.0 with HCl.
4. Finally, bring the volume to 2.47 mL for a final concentration of 10 mM.

Lovastatin (10 μM; 72 hours) efficiently reduces viability of HepG2 cells^[2].
Lovastatin (10 μM; 48 hours) induces apoptosis in HepG2 cells^[2]. In Vivo:Lovastatin is an inactive lactone that is hydrolyzed in the liver to an active f3-hydroxyacid form. This principal metabolite is the inhibitor of the enzyme HMG-CoA reductase. The K_i is 1 nM. Lovastatin and its β-hydroxyacid metabolite are highly bound to human plasma proteins. Lovastatin crosses the blood-brain and placental barriers^[3]. Lovastatin produces a profound reduction of apolipoprotein-B-containing lipoproteins, especially LDL cholesterol and, to a lesser extent, plasma triglycerides, and a small increase in HDL cholesterol^[4].