Fluvastatin (sodium salt hydrate) |
| カタログ番号GC47367 |
HMG-CoA還元酵素阻害剤
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: N/A
Sample solution is provided at 25 µL, 10mM.
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Fluvastatin is an inhibitor of HMG-CoA reductase (Ki = 0.3 nM for the rat enzyme) that binds to the HMG-CoA binding site.1,2 It also inhibits the human cytochrome P450 (CYP) isoform CYP2C9 (IC50 = 100 nM).3 Fluvastatin (2 mg/kg per day) inhibits increases in serum cholesterol, triglycerides, phospholipids, and thiobarbituric acid-reactive substances (TBARS) levels, as well as vascular angiotensin converting enzyme (ACE) activity in rabbits fed a high-cholesterol diet.4 It increases survival in a mouse model of myocardial infarction when administered at a dose of 10 mg/kg per day.5 Formulations containing fluvastatin have been used in the treatment of hypercholesterolemia and the prevention of cardiovascular disease.
1.Istvan, E.S., and Deisenhofer, J.Structural mechanism for statin inhibition of HMG-CoA reductaseScience292(5519)1160-1164(2001) 2.Corsini, A., Maggi, F.M., and Catapano, A.L.Pharmacology of competitive inhibitors of HMG-CoA reductasePharmacol. Res.31(1)9-27(1995) 3.Transon, C., Leemann, T., and Dayer, P.In vitro comparative inhibition profiles of major human drug metabolising cytochrome P450 isozymes (CYP2C9, CYP2D6 and CYP3A4) by HMG-CoA reductase inhibitorsEur. J. Clin. Pharmacol.50(3)209-215(1996) 4.Mitani, H., Bandoh, T., Ishikawa, J., et al.Inhibitory effects of fluvastatin, a new HMG-CoA reductase inhibitor, on the increase in vascular ACE activity in cholesterol-fed rabbitsBr. J. Pharmacol.119(6)1269-1275(1996) 5.Hayashidani, S., Tsutsui, H., Shiomi, T., et al.Fluvastatin, a 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor, attenuates left ventricular remodeling and failure after experimental myocardial infarctionCirculation105(7)868-873(2002)
| Cas No. | N/A | SDF | |
| Canonical SMILES | FC1=CC=C(C=C1)C2=C(/C=C/C(O)CC(O)CC([O-])=O)N(C(C)C)C3=C2C=CC=C3.[Na+].O | ||
| Formula | C24H25FNO4.Na [XH2O] | M.Wt | 410.5 |
| 溶解度 | DMF: 10 mg/ml,DMSO: 10 mg/ml,Ethanol: 0.5 mg/ml,PBS (pH 7.2): 0.2 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4361 mL | 12.1803 mL | 24.3605 mL |
| 5 mM | 0.4872 mL | 2.4361 mL | 4.8721 mL |
| 10 mM | 0.2436 mL | 1.218 mL | 2.4361 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
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