| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Fluvastatin targets HMG-CoA reductase (HMGCR), the rate-limiting enzyme in the mevalonate pathway of cholesterol biosynthesis. By competitively inhibiting HMGCR, Fluvastatin reduces the conversion of HMG-CoA to mevalonate, leading to decreased cholesterol synthesis in the liver and compensatory upregulation of LDL receptors, which enhances clearance of LDL cholesterol from the bloodstream. Fluvastatin also has pleiotropic effects on autophagy and inflammation.
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| ln Vitro |
In vitro, Fluvastatin sodium inhibits HMG-CoA reductase with an IC50 of 8 nM. Fluvastatin reduces cholesterol synthesis in cultured hepatocytes, leading to increased LDL receptor expression. It also induces autophagy and has anti-inflammatory effects by reducing the production of pro-inflammatory cytokines. The compound inhibits cell proliferation in some cancer cell lines. The deuterated form (d6) has identical biological activity to the unlabeled compound.
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| ln Vivo |
In vivo, Fluvastatin sodium lowers plasma cholesterol levels and prevents cardiovascular disease in animal models and humans. The deuterated form (d6) is not administered in vivo for therapeutic purposes but serves as an internal standard. Fluvastatin reduces total cholesterol, LDL cholesterol, and triglycerides while increasing HDL cholesterol. It also has beneficial effects on endothelial function and reduces cardiovascular events in patients with hypercholesterolemia.
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| Enzyme Assay |
Cell-free binding assays: Incubate purified HMG-CoA reductase (1-10 nM) with increasing concentrations of Fluvastatin-d6 sodium (0.1-1000 nM) in assay buffer (50 mM KPi, pH 7.4, 100 mM KCl, 1 mM EDTA, 1 mM DTT). Add the substrate HMG-CoA (10-100 uM) and cofactor NADPH (100 uM). Initiate the reaction by adding HMG-CoA. Measure NADPH consumption by absorbance at 340 nm over 5-15 minutes. Alternatively, use a coupled enzyme assay. Calculate IC50 and Ki by nonlinear regression. For isotopic use, prepare a calibration curve with unlabeled Fluvastatin and a fixed concentration of Fluvastatin-d6 as internal standard. Analyze by LC-MS/MS in negative ion mode: m/z 410.2 → 344.2 (unlabeled) and m/z 416.2 → 350.2 (d6).
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| Cell Assay |
Culture primary rat hepatocytes or human hepatoma cell lines (e.g., HepG2) in DMEM with 10% FBS. Treat cells with Fluvastatin-d6 sodium (1 nM-10 uM) for 6-48 hours. For cholesterol synthesis assays, add 14C-acetate or 3H-mevalonate to the medium, incubate for 2-4 hours, and measure incorporation into sterols by lipid extraction and scintillation counting. For LDL receptor expression, treat cells with Fluvastatin (0.1-10 uM for 24 hours), then perform Western blot for LDLR. Assess cell viability by MTT. For autophagy studies, treat with Fluvastatin (10 uM, 24 hours) and measure LC3-II/I ratio and p62 levels by Western blot. For inflammation assays, treat with Fluvastatin (0.1-10 uM) for 1 hour followed by LPS (1 ug/mL) for 6 hours, then measure TNF-alpha and IL-6 by ELISA.
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| Animal Protocol |
Animal studies are not typically performed with Fluvastatin-d6 itself as it is used as an analytical standard. For PK studies of Fluvastatin, administer unlabeled Fluvastatin sodium to rats or dogs via oral gavage (1-10 mg/kg) or intravenous injection (0.5-2 mg/kg). Collect blood at multiple time points (0-24 hours). Harvest plasma, add Fluvastatin-d6 sodium as internal standard, perform protein precipitation with acetonitrile, and analyze by LC-MS/MS. Calculate PK parameters including Cmax, Tmax, AUC0-t, AUC0-∞, t1/2, clearance, volume of distribution, and oral bioavailability. For efficacy studies, use hyperlipidemic animal models (e.g., high-fat diet-fed rats or LDLR-/- mice). Administer Fluvastatin (1-10 mg/kg/day, oral, 2-8 weeks). Measure plasma lipid profiles (total cholesterol, LDL, HDL, triglycerides) by enzymatic assays. Assess atherosclerosis by en face analysis of the aorta or by quantifying aortic root lesions after Oil Red O staining. For pharmacodynamic studies, harvest liver tissue at the end of treatment for HMGCR activity assays, LDLR mRNA expression by qPCR, and protein levels by Western blot.
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| ADME/Pharmacokinetics |
Fluvastatin-d6 sodium has a molecular weight of 439.48 and formula C24H19D6FNNaO4. The deuterated form is used as an internal standard for LC-MS/MS. Fluvastatin itself is rapidly absorbed after oral administration, with Cmax reached within 0.5-2 hours. It undergoes extensive first-pass metabolism (oral bioavailability ~20-30% in humans). Fluvastatin is metabolized primarily by CYP2C9 (with minor contributions from CYP2C8 and CYP3A4). The terminal half-life is approximately 1-2 hours in humans. The compound is highly protein-bound (>98%). Excretion occurs primarily in feces via biliary elimination. The d6 label does not significantly alter the PK profile due to minimal kinetic isotope effects. Solubility: H2O 50 mg/mL (113.77 mM), DMSO 50 mg/mL (113.77 mM). Storage: Powder at -20degC (3 years) or 4degC (2 years); in solvent at -80degC (6 months) or -20degC (1 month). Protect from light and moisture.
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| Toxicity/Toxicokinetics |
Fluvastatin sodium is generally well-tolerated in clinical use. Common adverse effects include myalgia, elevated liver transaminases, and gastrointestinal disturbances. Serious adverse effects include myopathy and rhabdomyolysis (rare). The deuterated form (d6) is not intended for in vivo administration; it is an analytical standard. For the unlabeled compound, hepatotoxicity is dose-dependent. Fluvastatin is contraindicated in pregnancy and in patients with active liver disease. No specific toxicity data for Fluvastatin-d6 are available. As an analytical standard, it is considered safe for laboratory use under standard chemical safety guidelines. Standard laboratory precautions (gloves, lab coat, safety glasses) should be used. Avoid inhalation and ingestion. The compound is not classified as hazardous for transport. In case of accidental exposure, wash affected area with soap and water. Dispose of waste according to institutional guidelines.
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| Additional Infomation |
Fluvastatin-d6 sodium is a stable isotope-labeled compound used as an internal standard for the accurate quantification of Fluvastatin in biological matrices by LC-MS/MS or GC-MS. Fluvastatin sodium (XU 62-320) was the first fully synthetic statin approved by the FDA (1993). It is marketed under brand names including Lescol and Lescol XL for the treatment of hypercholesterolemia and the prevention of cardiovascular events. Fluvastatin is less potent than some other statins (atorvastatin, rosuvastatin) but has a favorable drug-drug interaction profile due to its CYP2C9 metabolism. The d6 label has six deuterium atoms on the isopropyl group. The compound is for research use only and not for human diagnostic or therapeutic applications.
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| Molecular Formula |
C24H19D6FNNAO4
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| Molecular Weight |
439.48
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| Related CAS # |
Fluvastatin;93957-54-1;Fluvastatin sodium;93957-55-2;(3S,5R)-Fluvastatin-d6 sodium;2249799-35-5;(3S,5R)-Fluvastatin sodium;94061-81-1
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| Appearance |
Typically exists as solid at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2754 mL | 11.3771 mL | 22.7542 mL | |
| 5 mM | 0.4551 mL | 2.2754 mL | 4.5508 mL | |
| 10 mM | 0.2275 mL | 1.1377 mL | 2.2754 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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