Rosuvastatin

Modify Date: 2024-01-03 00:08:13

Rosuvastatin Structure
Rosuvastatin structure
 Common Name Rosuvastatin
CAS Number 287714-41-4 Molecular Weight 481.54
Density 1.368 g/cm3 Boiling Point 745.6ºC at 760 mmHg
Molecular Formula C22H28FN3O6S Melting Point N/A
MSDS N/A Flash Point 404.7ºC

 Use of Rosuvastatin


Rosuvastatin is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM. IC50 Value: 11 nM [1]Target: HMG-CoA reductasein 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].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].

 Names

Name rosuvastatin
Synonym More Synonyms

 Rosuvastatin Biological Activity

Description Rosuvastatin is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM. IC50 Value: 11 nM [1]Target: HMG-CoA reductasein 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].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].
Related Catalog
References

[1]. Watanabe, M., et al., Synthesis and biological activity of methanesulfonamide pyrimidine- and N-methanesulfonyl pyrrole-substituted 3,5-dihydroxy-6-heptenoates, a novel series of HMG-CoA reductase inhibitors. Bioorg Med Chem, 1997. 5(2): p. 437-44.

[2]. Schneck, D.W., et al., The effect of gemfibrozil on the pharmacokinetics of rosuvastatin. Clin Pharmacol Ther, 2004. 75(5): p. 455-63.

[3]. Kim, Y.S., et al., Rosuvastatin suppresses the inflammatory responses through inhibition of c-Jun N-terminal kinase and Nuclear Factor-kappaB in endothelial cells. J Cardiovasc Pharmacol, 2007. 49(6): p. 376-83.

[4]. Carswell, C.I., G.L. Plosker, and B. Jarvis, Rosuvastatin. Drugs, 2002. 62(14): p. 2075-85; discussion 2086-7.

[5]. Stalker, T.J., A.M. Lefer, and R. Scalia, A new HMG-CoA reductase inhibitor, rosuvastatin, exerts anti-inflammatory effects on the microvascular endothelium: the role of mevalonic acid. Br J Pharmacol, 2001. 133(3): p. 406-12.

 Chemical & Physical Properties

Density 1.368 g/cm3
Boiling Point 745.6ºC at 760 mmHg
Molecular Formula C22H28FN3O6S
Molecular Weight 481.54
Flash Point 404.7ºC
PSA 152.13000
LogP 2.14780
Vapour Pressure 2.38E-23mmHg at 25°C
Index of Refraction 1.597
Storage condition 2-8°C

 Synthetic Route

 Synonyms

Reference source: Negwer
volume-3 compound no
ROSUVASTATIN-D3 SODIUM SALT
7-[4-(4-Fluorophenyl)-6-(1-methylethyl)-2-(methyl-methylsulfonyl-amino)-pyrimidin-5-yl]-3,5-dihydroxy-hept-6-enoic acid
6-Heptenoic acid, 7-[4-(4-fluorophenyl)-6-(1-methylethyl)-2-[methyl-d(methylsulfonyl)amino]-5-pyrimidinyl]-3,5-dihydroxy-, sodium salt, (3R,5S,6E)- (1:1)
[3H]-Rosuvastatin
Rosuvastatin
Sodium (3R,5S,6E)-7-{4-(4-fluorophenyl)-6-isopropyl-2-[(H)methyl(methylsulfonyl)amino]-5-pyrimidinyl}-3,5-dihydroxy-6-heptenoate
(3R,5S,6E)-7-[4-(4-fluorophenyl)-2-(N-MethylMethanesulfonaMido)-6-(propan-2-yl)pyriMidin-5-yl]-3,5-dihydroxyhept-6-enoic acid
MFCD08460959
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