• 生物活性

靶点及简介 ：

Rosuvastatin is a potent HMG-CoA reductase inhibitor. Formulations containing rosuvastatin reduce low-density lipoprotein (LDL) and C-reactive protein and increase high-density lipoprotein (HDL) in humans.

罗舒伐他汀是HMG-CoA还原酶的抑制剂，其Ki值（抑制常数）约为0.1nM；HMG-CoA还原酶是催化胆固醇生物合成中的一种限速酶。

• 验证及参考文献

参考文献：

[1]. Watanabe, M., et al., Synthesis and biological activity of methanesulfonamide pyrimidine- and N-methanesulfonyl pyrrole-substituted 3,5-dihydroxy-6-heptenoates, a novel series of HMG-CoA reductase inhibitors. Bioorg Med Chem, 1997. 5(2): p. 437-44.

[2]. Schneck, D.W., et al., The effect of gemfibrozil on the pharmacokinetics of rosuvastatin. Clin Pharmacol Ther, 2004. 75(5): p. 455-63.

[3]. Kim, Y.S., et al., Rosuvastatin suppresses the inflammatory responses through inhibition of c-Jun N-terminal kinase and Nuclear Factor-kappaB in endothelial cells. J Cardiovasc Pharmacol, 2007. 49(6): p. 376-83.

[4]. Carswell, C.I., G.L. Plosker, and B. Jarvis, Rosuvastatin. Drugs, 2002. 62(14): p. 2075-85; discussion 2086-7.

[5]. Stalker, T.J., A.M. Lefer, and R. Scalia, A new HMG-CoA reductase inhibitor, rosuvastatin, exerts anti-inflammatory effects on the microvascular endothelium: the role of mevalonic acid. Br J Pharmacol, 2001. 133(3): p. 406-12.

• 溶解度及制备方案
  

  Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
  1 mM	2.08 mL	10.38 mL	20.77 mL
  5 mM	0.42 mL	2.08 mL	4.15 mL
  10 mM	0.21 mL	1.04 mL	2.08 mL
  50 mM	0.04 mL	0.21 mL	0.42 mL