344095-M

Fluvastatin, Sodium Salt

A synthetic HMG-CoA reductase inhibitor (IC₅₀ = 40-100 nM for human liver microsomes) that acts as an anti-hypercholesterolemic agent.

• Sinônimo(s): Fluvastatin, Sodium Salt, (±)-(3Rʹ,5Sʹ,6E)-7-[3-(4-Fluorophenyl)-1-isopropylindol-2-yl]-3,5-dihydroxy-6-heptenoate, sodium
• Fórmula empírica (Notação de Hill): C₂₄H₂₅FNNaO₄
• Número CAS: 93957-55-2
• Peso molecular: 433.45
• Número MDL: MFCD08063391
• Código UNSPSC: 12352200

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥98% (HPLC)
• forma: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: light yellow
• solubilidade: water: 30 mg/mL; DMSO: soluble; methanol: soluble
• temperatura de armazenamento: −20°C
• 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
• chave InChI: ZGGHKIMDNBDHJB-RPQBTBOMSA-M

Descrição

Descrição geral

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.

Ações bioquímicas/fisiológicas

Primary Target
HMG-CoA reductase

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

Advertência

Toxicity: Carcinogenic / Teratogenic (D)

Reconstituição

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

Outras notas

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.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable