General description
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-Dealkylation and β-oxidation of the side-chain also occurs. The hydroxy metabolites are also reported to have some pharmacologic activity.
Biochem/physiol Actions
Reversible: yes
Packaging
Packaged under inert gas
Other Notes
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | liquid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,avoid repeated freeze/thaw cycles,protect from light |
| shipped in | dry ice |
| storage temp. | −70°C |
| SMILES string | [Na+].Fc1ccc(cc1)c2c3c([n](c2\C=C\[C@H](O)C[C@H](O)CC(=O)[O-])C(C)C)cccc3 |
| InChI | 1S/C24H26FNO4.Na/c1-15(2)26-21-6-4-3-5-20(21)24(16-7-9-17(25)10-8-16)22(26)12-11-18(27)13-19(28)14-23(29)30;/h3-12,15,18-19,27-28H,13-14H2,1-2H3,(H,29,30);/q;+1/p-1/b12-11+;/t18-,19-;/m0./s1 |
| InChI key | ZGGHKIMDNBDHJB-RPQBTBOMSA-M |
