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Rosuvastatin/瑞舒伐他汀 {[allProObj[0].p_purity_real_show]}

货号:A101253 同义名: 罗伐他汀 / ZD 4522

Rosuvastatin is a synthetic and highly effective statin-class HMG-CoA reductase inhibitor with IC50 of 11 nM.

Rosuvastatin/瑞舒伐他汀 化学结构 CAS号:287714-41-4
Rosuvastatin/瑞舒伐他汀 化学结构
CAS号:287714-41-4
Rosuvastatin/瑞舒伐他汀 3D分子结构
CAS号:287714-41-4
Rosuvastatin/瑞舒伐他汀 化学结构 CAS号:287714-41-4
Rosuvastatin/瑞舒伐他汀 3D分子结构 CAS号:287714-41-4
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Rosuvastatin/瑞舒伐他汀 纯度/质量文件 产品仅供科研

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Rosuvastatin/瑞舒伐他汀 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]

Rosuvastatin/瑞舒伐他汀 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 <<

Rosuvastatin/瑞舒伐他汀 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

Rosuvastatin/瑞舒伐他汀 实验方案

计算器
存储液制备 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

Rosuvastatin/瑞舒伐他汀 技术信息

CAS号287714-41-4
分子式C22H28FN3O6S
分子量 481.54
SMILES Code O=C(O)C[C@H](O)C[C@H](O)/C=C/C1=C(C(C)C)N=C(N(C)S(=O)(C)=O)N=C1C2=CC=C(F)C=C2
MDL No. MFCD18783208
别名 罗伐他汀 ;ZD 4522
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C

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