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Rosuvastatin Calcium
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Rosuvastatin Calcium图片
CAS NO:147098-20-2
规格:≥98%
包装与价格:
包装价格(元)
250mg电议
500mg电议
1g电议
2g电议
5g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)500.57
FormulaC22H28FN3O6S.1/2Ca
CAS No.147098-20-2 (calcium);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 100 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)4% DMSO+30% PEG 300+dd H2O: 10 mg/mL
SynonymsZD 4522; Rosuvastatin calcium; S-4522; Rosuvastatin hemicalcium; ZD-4522; ZD4522; S 4522; S4522; ZD 4522 calcium salt; ZD 4522 Calcium; Brand name: Crestor.
Chemical Namecalcium (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoate
SMILES CodeCC(C1=NC(=NC(=C1/C=C/C(O)CC(O)CC(=O)[O-])C2=CC=C(C=C2)F)N(S(=O)(=O)C)C)C.CC(C1=NC(=NC (=C1/C=C/C(O)CC(O)CC(=O)[O-])C2=CC=C(C=C2)F)N(S(=O)(=O)C)C)C.[Ca+2]
实验参考方法
In Vitro

In vitro activity: Rosuvastatin is relatively hydrophilic and is highly selective for hepatic cells; its uptake is mediated by the liver-specific organic anion transporter OATP-C. Rosuvastatin is a high-affinity substrate for OATP-C with apparent association constant of 8.5 μM. Rosuvastatin inhibits cholesterol biosynthesis in rat liver isolated hepatocytes with IC50 of 1.12 nM. Rosuvastatin causes approximately 10 times greater increase of mRNA of LDL receptors than pravastatin. Rosuvastatin (100 μM) decreases the extent of U937 adhesion to TNF-α-stimulated HUVEC. Rosuvastatin inhibits the expressions of ICAM-1, MCP-1, IL-8, IL-6, and COX-2 mRNA and protein levels through inhibition of c-Jun N-terminal kinase and nuclear factor-kB in endothelial cells.


Kinase Assay: Rosuvastatin Calcium is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM.


Cell Assay: Rosuvastatin is relatively hydrophilic and is highly selective for hepatic cells; its uptake is mediated by the liver-specific organic anion transporter OATP-C. Rosuvastatin is a high-affinity substrate for OATP-C with apparent association constant of 8.5 μM. Rosuvastatin inhibits cholesterol biosynthesis in rat liver isolated hepatocytes with IC50 of 1.12 nM. Rosuvastatin causes approximately 10 times greater increase of mRNA of LDL receptors than pravastatin. Rosuvastatin (100 μM) decreases the extent of U937 adhesion to TNF-α-stimulated HUVEC. Rosuvastatin inhibits the expressions of ICAM-1, MCP-1, IL-8, IL-6, and COX-2 mRNA and protein levels through inhibition of c-Jun N-terminal kinase and nuclear factor-kB in endothelial cells.

In VivoRosuvastatin is efficient on reducing plasma liquids. Rosuvastatin (3 mg/kg) daily administration for 14 days decreases plasma cholesterol levels by 26% in male beagle dogs with normal cholesterol levels. In cynomolgus monkeys, Rosuvastatin decreases plasma cholesterol levels by 22% Rosuvastatin (20 mg/kg/day) administration for 2 weeks, significantly reduces very low-density lipoproteins (VLDL) in diabetes mellitus rats induced by Streptozocin. Rosuvastatin shows antiatherothromhotic effects in vivo. Rosuvastatin (1.25 mg/kg) significantly inhibits thrombin-induced transmigration of monocvtes across mesenteric venules via inhibition of the endothelial cell surface expression of P-selectin, and increases the basal rate of nitric oxide in aortic segments by 2-fold times. Rosuvastatin (20 mg/kg) inhibits ROS production, normalizes NO-dependent endothelial function and reduces platelet activation in diabetic rats induced by Streptozocin. Rosuvastatin displays cardioprotective effects in vivo. Rosuvastatin (80 mg) is shows to decrease infarct size and improve cardiac mechanical function after ischemia/reperfusion in animal model. The cardioprotective properties of Rosuvastatin may be due to the improvement of coronary blood flow, decrease in resistance of coronary arteries mediated by enhanced eNOS expression, and the subsequent increase in the production of vascular endothelial NO. Rosuvastatin (2.0 mg/kg) attenuates left ventricular hypertrophy produced by transaortic constriction in mice through regulation of Racl protein and NADPH oxidase activities.
Animal modelMale beagle dogs and Monkey
Formulation & Dosage 20 mg/kg/day
ReferencesClin Pharmacol Ther. 2004 May;75(5):455-63; Bioorg Med Chem. 1997 Feb;5(2):437-44.