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Rosuvastatin Calcium

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Chemical Structure| 147098-20-2 同义名 : Rosuvastatin hemicalcium;ZD 4522 Calcium;ZD 4522;Rosuvastatin (calcium salt)
CAS号 : 147098-20-2
货号 : A272688
分子式 : C44H54CaF2N6O12S2
纯度 : 98%
分子量 : 1001.137
MDL号 : MFCD04112702
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(24.97 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 1 mg/mL(1 mM)，配合低频超声助溶
动物实验配方：

4% DMSO+30% PEG 300+dd water 10 mg/mL

生物活性
描述 HMG-CoA reductase (HMGCR) catalyzes the rate-limiting step in cholesterol biosynthesis. Rosuvastatin calcium is a potent inhibitor of HMGCR with an Ki value of 0.1 nM and an IC50 value of 5.4 nM. The cholesterol synthesis in hepatocytes was inhibited by rosuvastatin calcium with an IC50 value of 0.2 nM. Rosuvastatin calcium also shows high affinity for liver-specific organic anio transport proteins (OATPs). The apparent Km value for the interaction between rosuvastatin calcium and OATP-C was 7.3 μM[3]. In papillary thyroid carcinoma B-CPAP cells, rosuvastatin calcium at 12.5 – 200 μM decreased cell viability with IC50 values of 12.9 μM and 4.6 μM for 48h- and 72h- incubations, respectively. Treatment with 50 μM rosuvastatin calcium for 48 hours led to G1 phase arrest in B-CPAP cells with a subG1 cell peak. Rosuvastatin calcium at 12.5 – 200 μM also caused a gradual decrease in the number of B-CPAP cells and an increase of the number of vacuoles at a dose-dependent manner. The caspase-3 activity and apoptotic rate in B-CPAP cells were significantly increased by rosuvastatin calcium at 12.5 μM[4]. Oral administration of rosuvastatin calcium in rats inhibited hepatic cholesterol synthesis with an ED50 of 0.8 mg/kg as measured 2 to 3 hours post treatment[3].
作用机制 Rosuvastatin calcium contains a dihydroxy heptenoic acid chain that mimics the HMG portion of HMGCR[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
NCT01241903 Acute Coronary Syndrome ... 展开 >> Angioplasty, Transluminal, Percutaneous Coronary Hydroxymethylglutaryl-CoA Reductase Inhibitors Blood Platelets 收起 << Phase 1 Completed - United States, Kentucky ... 展开 >> University of Kentucky Dept of Cardiology Lexington, Kentucky, United States, 40536 收起 <<
NCT01241903 - Completed - -
NCT00747149 Type 2 Diabetes Phase 4 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.00mL

0.20mL

0.10mL

4.99mL

1.00mL

0.50mL

9.99mL

2.00mL

1.00mL
参考文献

[1]Schneck DW, Birmingham BK, et al. The effect of 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-methanesulfonylpyrrole-substituted 3,5-dihydroxy-6-heptenoates, a novel series of HMG-CoA reductase inhibitors. Bioorg Med Chem. 1997 Feb;5(2):437-44.

[3]Olsson AG, McTaggart F, Raza A. Rosuvastatin: a highly effective new HMG-CoA reductase inhibitor. Cardiovasc Drug Rev. 2002 Winter;20(4):303-28.

[4]Zeybek ND, Gulcelik NE, Kaymaz FF, Sarisozen C, Vural I, Bodur E, Canpinar H, Usman A, Asan E. Rosuvastatin induces apoptosis in cultured human papillary thyroid cancer cells. J Endocrinol. 2011 Jul;210(1):105-15.