Catalog No.S2169 Synonyms: ZD4522
Molecular Weight(MW): 500.57
Rosuvastatin Calcium is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM in a cell-free assay.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|Description||Rosuvastatin Calcium is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM in a cell-free 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 vivo||Rosuvastatin 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. |
-  Schneck DW, et al. Clin Pharmacol Ther, 2004, 75(5), 4554-63.
-  Watanabe M, et al. Bioorg Med Chem, 1997, 5(2), 437-444.
-  Kim YS, et al. J Cardiovasc Pharmacol, 2007, 49(6), 376-383.
-  Carswell CI, et al. Drugs, 2002, 62(14), 2075-2085
-  Stalker TJ, et al. Br J Pharmacol, 2001, 133(3), 406-412.
-  Sch?fer A, et al. Biochem Pharmacol, 2007, 73(9), 1367-1375.
-  Bulhak AA, et al. Acta Physiol Scand, 2005, 183(2), 151-159.
-  Custodis F, et al. Cardiovasc Res, 2006 Jul 15, 71(2), 342-351.
-  Dansette PM, et al. Exp Toxicol Pathol, 2000, 52(2), 145-148.
|In vitro||DMSO||100 mg/mL warmed (199.77 mM)|
|In vivo||4% DMSO+30% PEG 300+dd H2O||10mg/mL|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02740699||Recruiting||Cardiovascular Disease||National Institutes of Health Clinical Center (CC)||April 4, 2016||Phase 4|
|NCT02995720||Active, not recruiting||Hypertension, Hyperlipidemia||Boryung Pharmaceutical Co., Ltd||August 26, 2016||Phase 1|
|NCT02662894||Not yet recruiting||Hypertension|Dyslipidemia||EMS||July 2017||Phase 3|
|NCT02901067||Not yet recruiting||Wounds and Injuries|Venous Thromboembolism||Denver Health and Hospital Authority||January 2017||Phase 2|
|NCT02977065||Not yet recruiting||Dyslipidemias||Chong Kun Dang Pharmaceutical||January 2017||Phase 2|
|NCT03010475||Recruiting||Diabetes|Healthy||Novo Nordisk A/S||January 2017||Phase 1|
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