Rosuvastatin
CAS No. | 287714-41-4 | Cat. No. | BCP02356 |
Name | Rosuvastatin | ||
Synonyms | S-4522; S 4522; S4522; ZD 4522;ZD-4522;ZD4522;X-Plended;Crestor; | ||
Formula | C22H28FN3O6S | M. Wt | 481.54 |
Description | 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 . 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 (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% . R | ||
Pathways | Protease/Metabolic Enzyme | ||
Targets | HMGCR |
Structure
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