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| Cas No.: | 147098-20-2 |
| Chemical Name: | calcium (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoate |
| Synonyms: | S-4522; S 4522; S4522; ZD 4522; ZD-4522; ZD4522; ZD 4522 calcium salt; Rosuvastatin calcium, trade name: Crestor. |
| SMILES: | CC(C)C1=C(/C=C/[C@@H](O)C[C@@H](O)CC([O-])=O)C(C2=CC=C(F)C=C2)=NC(N(C)S(C)(=O)=O)=N1.CC(C)C3=C(/C=C/[C@@H](O)C[C@@H](O)CC([O-])=O)C(C4=CC=C(F)C=C4)=NC(N(C)S(C)(=O)=O)=N3.[Ca+2] |
| Formula: | C44H54CaF2N6O12S |
| M.Wt: | 1001.14 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | Rosuvastatin Calcium is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM. |
| In Vivo: | 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% [1]. Rosuvastatin (20 mg/kg/day) administration for 2 weeks, significantly reduces very low-density lipoproteins (VLDL) in diabetes mellitus rats induced by Streptozocin [4]. 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 [5]. |
| In Vitro: | 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 [2]. 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 [1]. 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 [3]. |