HMG-CoA reductase inhibitor,highly selective and competitive
CAS：81131-70-6
分子式：C23H35O7.Na
分子量：446.51
纯度：98%
存储：Store at -20°C

Background:

Pravastatin sodium is a high selective inhibitor of 3-hydroxy-3-methylglutaryl coenzyme-A (HMG-CoA) reductase of 44.1nM [1].

Pravastatin is a competitive inhibitor of HMG-CoA reductase. It has shown to reduce the level of plasma LDL both in animals and humans through inhibiting cellular cholesterol synthesis. Pravastatin was reported to reduce cellular cholesterol synthesis in three types of macrophages including J-774 A.1 macrophage-like cell line, human monocyte derived macrophages (HMDM) and mouse peritoneal macrophages (MPM) with IC50 values of 0.08, 6.3 and 7.8μg/ml, respectively [2].

Besides the benefit in cardiovascular disease prevention, pravastatin also has efficacy of preventing tumor growth in some degree. However, it has shown that the normal hepatocytes are more sensitive to pravastatin than the tumor cells since pravastatin is selectively taken up by OATP1B1 which is exclusively expressed in normal hepatocytes [3].

参考文献:
[1] Bolego C, Poli A, Cignarella A, Catapano AL, Paoletti R. Novel statins: pharmacological and clinical results. Cardiovasc Drugs Ther. 2002 May;16(3):251-7.
[2] Keidar S, Aviram M, Maor I, Oiknine J, Brook JG. Pravastatin inhibits cellular cholesterol synthesis and increases low density lipoprotein receptor activity in macrophages: in vitro and in vivo studies. Br J Clin Pharmacol. 1994 Dec;38(6):513-9.
[3] Menter DG, Ramsauer VP, Harirforoosh S, Chakraborty K, Yang P, Hsi L, Newman RA, Krishnan K. Differential effects of pravastatin and simvastatin on the growth of tumor cells from different organ sites. PLoS One. 2011;6(12):e28813.