product name Fluvastatin Sodium
Description: Fluvastatin (also known as XU-62-320) belongs to a class of medications called statins, it inhibits HMG-CoA reductase activity with IC50 of 8 nM in a cell-free assay and is used to reduce plasma cholesterol levels and prevent cardiovascular disease. It is also the first entirely synthetic HMG-CoA reductase inhibitor and is structurally distinct from the fungal derivatives of this therapeutic class.
References: Exp Toxicol Pathol. 2000 May;52(2):145-8; J Pharm Pharmacol. 2001 Feb;53(2):227-32.
433.45
Formula
C24H25FNNaO4
CAS No.
93957-55-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 87 mg/mL (200.7 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
Synonyms
XU-62-320
other peoduct :
| In Vitro |
In vitro activity: Fluvastatin markedly inhibits the formation of thiobarbituric acid reactive substances in iron (II)-supported peroxidation of liposomes with IC50 of 12 μM. Fluvastatin ranging from 1 μM to 100 μM inhibits peroxyl radical-mediated peroxidation of liposomes induced by water-soluble and lipid-soluble radical generators, 2,2-azobis (2-amidinopropane) dihydro-chloride and 2,2-azobis (2,4-dimethylvaleronitrile), respectively. Fluvastatin (4 mM) and its metabolites shows superoxide anion scavenging activity in the hypoxanthine-xanthine oxidase system and a strong scavenging effect on the hydroxyl radical produced from Fentons reaction. Fluvastatin (8 μM) and its metabolites shows protective effects on DNA damage as potent as the reference antioxidants, ascorbic acid, trolox, and probucol in CHL/IU cells. Fluvastatin (100 nM) shows a dose-dependent decrease in Ang II-activated superoxide anion formation in human aortic smooth muscle cells (hASMC). Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Fluvastatin (10 mg/kg/day) results in a decrease in serum lipids in rabbits feed a 1.5% cholesterol containing diet. Fluvastatin (10 mg/kg/day) significantly lowers the tissue ACE in the aortae in rabbits feed a 1.5% cholesterol containing diet. Fluvastatin (10 mg/kg/day) significantly reverses the suppression of ACh-induced relaxation in rabbits feed a 1.5% cholesterol containing diet. |
| Animal model | Male Japanese white rabbits |
| Formulation & Dosage | Dissolved in saline; 10 mg/kg; taken with diet |
| References | Exp Toxicol Pathol. 2000 May;52(2):145-8; J Pharm Pharmacol. 2001 Feb;53(2):227-32; Br J Pharmacol. 1996 Nov;119(6):1269-75. |
