Fluvastatin, Sodium Salt

A synthetic HMG-CoA reductase inhibitor (IC₅₀ = 40-100 nM for human liver microsomes) that acts as an anti-hypercholesterolemic agent. Decreases the basal MMP-1 levels in culture media of endothelial cells in a time- and dose-dependent manner. Inhibits the formation of TBA-reactive substances in Fe(II)-supported peroxidation of liposomes (IC₅₀ = 12 µM). Also available as a 10 mM solution in H₂O(Cat. No. 344096).

A synthetic, competitive inhibitor of HMG-CoA reductase that acts as anti-hypercholesterolemic agent. Unlike Lovastatin (Cat. No. 438185), Mevastatin (Cat. No. 474700), and Simvastatin (Cat. No. 567020), it does not require activation prior to use for in vitro studies. Reduces the basal MMP-1 levels in culture media of endothelial cells in a time- and dose-dependent manner. Fluvastatin is metabolized in the liver, primarily via hydroxylation of the indole ring at the 5- and 6-positions. N-Dealky-lation and b-oxidation of the side-chain also occurs. The hydroxy metabolites are also reported to have some pharmacologic activity.

Primary Target
HMG-CoA reductase

Target IC₅₀: 40-100 nM against HMG-CoA reductase in human liver microsomes

Toxicity: Carcinogenic / Teratogenic (D)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Yamamoto, A., et al. 2001. J. Pharm. Pharmacol.53, 227.
Dansette, P.M., et al. 2000. Exp. Toxicol. Pathol.52, 145.
Ikeda, U., et al. 2000. Hypertension36, 325.
Levy, R.I., et al. 1993. Circulation87 (4 Suppl.), III45.
Tse, F.L.S. et al. 1992. J. Clin. Pharmacol.32, 630.
Yuan, J., et al. 1991. Atherosclerosis87, 147.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany