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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related HMG-CoA Reductase Products |
|---|
| Fluvastatin
Fluvastatin is the first fully synthesized, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM.Fluvastatin protects vascular smooth muscle cells from oxidative stress through an Nrf2-dependent antioxidant pathway. |
| Pravastatin lactone
Pravastatin lactone is a potent HMG-CoA inhibitor. |
| HMG-CoA Reductase-IN-1
HMG-CoA Reductase-IN-1 is a HMG-CoA reductase inhibitor. |
| Ganomycin I
Ganomycin I is a dual inhibitor of α-Glucosidase and HMG-CoA reductase. |
| Ganoderenic acid K
Ganoderenic acid K is a natural product, that can be isolated from fruiting bodies of Ganoderma lucidum. |
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