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.

• 別名: Fluvastatin, Sodium Salt, (±)-(3Rʹ,5Sʹ,6E)-7-[3-(4-Fluorophenyl)-1-isopropylindol-2-yl]-3,5-dihydroxy-6-heptenoate, sodium
• 実験式（ヒル表記法）: C₂₄H₂₅FNNaO₄
• CAS番号: 93957-55-2
• 分子量: 433.45
• MDL番号: MFCD08063391
• UNSPSCコード: 12352200

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: light yellow
• 溶解性: water: 30 mg/mL; DMSO: soluble; methanol: soluble
• 保管温度: −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
• InChI Key: ZGGHKIMDNBDHJB-RPQBTBOMSA-M

詳細

詳細

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.

生物化学的／生理学的作用

Primary Target
HMG-CoA reductase

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

警告

Toxicity: Carcinogenic / Teratogenic (D)

再構成

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

その他情報

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.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable