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Fluvastatin sodium is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonic acid. Fluvastatin markedly inhibits the formation of thiobarbituric acid reactive substances in iron (II)-supported peroxidation of liposomes with IC50 of 12 μM. Fluvastatin sodium inhibits vascular smooth muscle proliferation in vitro (IC50 = 70 nM) and exhibits antihypercholesterolemic and antioxidant activity in vivo. When fluvastatin was administered in a clinical trial to patients undergoing percutaneous coronary intervention, LDL cholesterol levels were reduced by 27% after six weeks of treatment with a dose of 40 mg/kg twice a day compared to placebo. Fluvastatin sodium is antilipemic and is used to reduce plasma cholesterol levels and prevent cardiovascular disease. Fluvastatin is currently in a phase IV clinical trial in patients with Metabolic Syndrome.
Pak J Pharm Sci. 2016 May;29(3 Suppl):1043-51.
Chromatographic resolution of drug analogues: 3-hydroxy-3-methylglutarylcoenzyme A reductase inhibitors (statins)
Fluvastatin sodium purchased from AbMole
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Source | Pak J Pharm Sci (2016). Figure 1. Fluvastatin sodium (Abmole Bioscience) |
| Method | HPLC chromatogram | |
| Cell Lines | ||
| Concentrations | 150μg/ml | |
| Incubation Time | ||
| Results | The results summarized in (table 1) obtained for pravastatin, rosuvastatin, pitavastatin, atorvastatin, fluvastatin, lovastatin and simvastatin were comparable with the corresponding labeled amounts. |
| Molecular Weight | 433.45 |
| Formula | C24H25FNNaO4 |
| CAS Number | 93957-55-2 |
| Solubility (25°C) | Water 45 mg/mL DMSO 45 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related HMG-CoA Reductase Products |
|---|
| Lovastatin
Lovastatin is an inhibitor of HMG-CoA reductase with IC50 of 3.4 nM in a cell-free assay, used for lowering cholesterol (hypolipidemic agent). |
| Rosuvastatin calcium
Rosuvastatin (Crestor) is a member of statins and used to treat high cholesterol and related conditions. |
| Mevastatin
Mevastatin is a competitive inhibitor of HMG-Coenzyme A (HMG-CoA) reductase with a binding affinity 10,000 times greater than the HMG-CoA substrate itself. |
| Pravastatin sodium
Pravastatin sodium is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM. |
| Clinofibrate
Clinofibrate inhibits hydroxymethylglutaryl coenzyme A reductase (HMGCR) with IC50 of 0.47 mM, is a lipid-lowering agent used for controlling high cholesterol and triacylglyceride levels in the blood. |
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