同义名 :	罗伐他汀 ;ZD 4522
	CAS号 :	287714-41-4
	货号 :	A101253
	分子式 :	C22H28FN3O6S
	纯度 :	99%
	分子量 :	481.54
	MDL号 :	MFCD18783208
	存储条件：	Pure form Sealed in dry, store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-

生物活性
描述	Rosuvastatin is a hydroxymethylglutaryl coenzyme A reductase inhibitor with an IC50 value of 11nM in vitro.[4] It blocked human ether-a-go-go related gene (hERG) current in HEK293 cells with an IC50 value of 195nM. In isolated guinea pig hearts, rosuvastatin at a concentration of 195nM prolonged the monophasic action potential duration at 90% repolarization by 11ms.[3] Rosuvastatin also inhibited cholesterol biosynthesis in isolated rat hepatocytes with an IC50 value of 0.16nmol/L. In mice with streptozocin-induced diabetes mellitus, rosuvastatin treatment at a dosage of 20 mg/kg/day for 2 weeks significantly reduced the level of very low-density lipoproteins.[5]
作用机制	Rosuvastatin is a methanesulfonamide derivative that acts as an inhibitor of hydroxymethylglutaryl coenzyme A reductase. It also shows structural similarities with several potassium current blockers and has been reported to blocks hERG current and prolongs cardiac repolarization.[3]

临床研究
NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02186483	Hyperlipidemia ... 展开 >> Diabetes 收起 <<	Phase 1	Completed	-	Korea, Republic of ... 展开 >> Samsung Medical Center(SMC) Seoul, Gangnam-Gu, Korea, Republic of, 135-710 收起 <<
NCT01411111	Asthma	Phase 1	Completed	-	United Kingdom ... 展开 >> GSK Investigational Site London, United Kingdom, NW10 7EW 收起 <<
NCT01101568	Diabetes Mellitus, Type 2	Phase 1	Completed	-	United States, Texas ... 展开 >> GSK Investigational Site Austin, Texas, United States, 78744 收起 <<

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.08mL 0.42mL 0.21mL	10.38mL 2.08mL 1.04mL	20.77mL 4.15mL 2.08mL

参考文献

[1]Schneck DW, Birmingham BK, et al. gemfibrozil on the pharmacokinetics of rosuvastatin. Clin Pharmacol Ther. 2004 May;75(5):455-63. [2]Watanabe M, Koike H, 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 Feb;5(2):437-44. [3]Plante I, Vigneault P, Drolet B, Turgeon J. Rosuvastatin blocks hERG current and prolongs cardiac repolarization. J Pharm Sci. 2012 Feb;101(2):868-78 [4]Watanabe M, Koike H, Ishiba T, Okada T, Seo S, Hirai K. 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 Feb;5(2):437-44 [5]Carswell CI, Plosker GL, Jarvis B. Rosuvastatin. Drugs. 2002;62(14):2075-85; discussion 2086-7