sodium:(E,3R,5S)-7-[4-(4-fluorophenyl)-6-(1,1,1,3,3,3-hexadeuteriopropan-2-yl)-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoate

Biological Activity

Rosuvastatin-d6 is intended for use as an internal standard for the quantification of rosuvastatin by GC- or LC-MS. Rosuvastatin is an HMG-CoA reductase inhibitor (IC50 = 5 nM).1,2 It is a fully-synthetic inhibitor that is designed to maximize the points of contact with, and inhibition of, HMG-CoA reductase.1 Formulations containing rosuvastatin reduce low-density lipoprotein and C-reactive protein and increase high-density lipoprotein in humans.3,4

References

1.Istvan, E.S., and Deisenhofer, J.Structural mechanism for statin inhibition of HMG-CoA reductaseScience292(5519)1160-1164(2001) 2.Tobert, J.A.Lovastatin and beyond: The history of the HMG-CoA reductase inhibitorsNat. Rev. Drug Discov.2(7)517-526(2003) 3.Asztalos, B.F., Maulf, F.L., Dallal, G.E., et al.Comparison of the effects of high doses of Rosuvastatin versus Atorvastatin on the subpopulations of high-density lipoproteinsAm. J. Cardiol.99(5)681-685(2007) 4.Rubba, P., Marotta, G., and Gentile, M.Efficacy and safety of rosuvastatin in the management of dyslipidemiaVasc. Health Risk Manag.5(1)343-352(2009)