HMG-CoA reductase inhibitor
Rosuvastatin is an inhibitor of HMG-CoA reductase, an enzyme that catalyzes the rate-limiting step in cholesterol biosynthesis, with Ki value (inhibition constant) of approximately 0.1 nM.
Rosuvastatin 100 mg
£355.00
Target: HMG-CoA reductase
Chemical name: 6-Heptenoic acid, 7-[4-(4-fluorophenyl)-6-(1-methylethyl)-2-[methyl(methylsulfonyl)amino]-5-pyrimidinyl]-3,5-dihydroxy-, (3R,5S,6E)-
Formula: C22H28FN3O6S
Molecular weight: 481.54
Purity: 98.4 %
Solubility: 32 mg/mL (DMSO); 96 mg/mL (water)
Size: 100 mg
Storage: 3 years -20°C powder, 2 years -80°C in solvent
In vitro:
Rosuvastatin possesses a greater number of binding interactions with HMG-CoA reductase and has a high affinity for the active site of the enzyme. Rosuvastatin is relatively hydrophilic and is selectively taken up by, and active in, hepatic cells. Rosuvastatin has the longest terminal half-life of the statins and is only minimally metabolized by the cytochrome P450 (CYP 450) enzyme system with no significant involvement of the 3A4 enzyme[2].
In vivo:
Rosuvastatin attenuates arterial thrombosis and neointima formation, and it may stabilise vascular lesions developing after endothelial injury in mice. These effects are independent of systemic lipid lowering[3].
References:
[1] Ikeda Y, et al. J Cardiovasc Pharmacol. 2003, 41(4):649-56.
[2] Rosenson RS. Expert Rev Cardiovasc Ther. 2003, 1(4):495-505.
[3] Schäfer K, et al. Thromb Haemost. 2005, 93(1):145-52.