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Introduction of 101314-97-0 :
Simvastatin sodium is a lactone prodrug, can be hydrolysed to active hydroxy-acid by non-specific carboxyesterases or non-enzymatic processes. Simvastatin sodium shows a inhibition of HMG-CoA reductase with a Ki value of 0.12 nM. In Vitro: Simvastatin sodium shows a inhibition of HMG-CoA reductase in human lymphoblasts and SV40 transformed MRCS fibroblasts. Simvastatin sodium (100 μM) inhibits the Na+/H+ antiport activity leading to a fall of intracellular pH and to a reduced cell proliferation.And the inhibitory effect is prevented by mevalonate but not dolichol or squalene. In Vivo: Simvastatin sodium (oral administration; 8 mg/kg; 18 days) reduces plasma cholesterol levels 33%, simvastatin can be used in combination with ezetimibe to treat dyslipidemia.