| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Fluvastatin (XU-62320; Fluindostatin; Lescol XL; XU-62-320; Canef; Lipaxan; Vastin), an approved drug belonging to the statin class of hypolipidemic medications, is a potent inhibitor of HMG-CoA reductase activity with potential anti-hyperlipidemic effects. It inhibits HMG-CoA reductase with an IC50 of 8 nM in a cell-free assay. Fluvastatin 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.
| ln Vitro |
The enzyme hydroxymethylglutaryl-coenzyme A reductase (HMGCR), which catalyzes the rate-limiting conversion of HMG-CoA to mevalonic acid in cholesterol biosynthesis, is competitively inhibited by fluvastatin sodium (XU 62320). Studies on HCC (human hepatocellular cancer cells) show that fluvastatin causes G2/M phase arrest. HCC cells display less Bcl-2 and procaspase-9 and more Bax, cleaved caspase-3, and cytochrome c when fluvastatin (XU 62320) is present. The antilipemic drug fluvastatin (XU 62320) lowers plasma cholesterol levels and prevents cardiovascular disease.
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| ln Vivo |
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| Animal Protocol |
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation No relevant published information exists on the use of fluvastatin during breastfeeding. Because of a concern with disruption of infant lipid metabolism, the consensus is that fluvastatin should not be used during breastfeeding. However, others have argued that children homozygous for familial hypercholesterolemia are treated with statins beginning at 1 year of age, that statins have low oral bioavailability, and risks to the breastfed infant are low, especially with rosuvastatin and pravastatin.[1] Until more data become available, an alternate drug may be preferred, especially while nursing a newborn or preterm infant. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
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| References |
[1]. Makabe S, et al. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway. Atherosclerosis. 2010 Dec;213(2):377-84.
[2]. Wu Zhang, et al. Fluvastatin, a lipophilic statin, induces apoptosis in human hepatocellular carcinoma cells through mitochondria-operated pathway. Indian J Exp Biol. 2010 Dec;48(12):1167-74. |
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| Additional Infomation |
Fluvastatin Sodium is the sodium salt of a synthetic lipid-lowering agent with potential antineoplastic activity. Fluvastatin competitively inhibits hepatic 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis. This agent lowers plasma cholesterol and lipoprotein levels, and modulates immune responses through the suppression of MHC II (major histocompatibility complex II) on interferon gamma-stimulated, antigen-presenting cells such as human vascular endothelial cells. Through the inhibition of mevalonate synthesis, statins, like fluvastatin, have been shown to inhibit the production of dolichol, geranylpyrophosphate (GPP) and farnesylpyrophosphate (FPP) and the isoprenylation of the intracellular G-proteins Ras and Rho, which may result in antiangiogenic, apoptotic, and antimetastatic effects in susceptible tumor cell populations.
An indole-heptanoic acid derivative that inhibits HMG COA REDUCTASE and is used to treat HYPERCHOLESTEROLEMIA. In contrast to other statins, it does not appear to interact with other drugs that inhibit CYP3A4. |
| Molecular Formula |
C24H25FNNAO4
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| Molecular Weight |
433.45
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| Exact Mass |
433.166
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| CAS # |
93957-55-2
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| Related CAS # |
Fluvastatin;93957-54-1;Fluvastatin-d6 sodium;(3S,5R)-Fluvastatin-d6 sodium;2249799-35-5;(3S,5R)-Fluvastatin sodium;94061-81-1
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| PubChem CID |
16760425
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| Appearance |
Typically exists as solid at room temperature
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| Boiling Point |
681.8ºC at 760 mmHg
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| Melting Point |
194-197ºC
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| LogP |
3.293
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
31
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| Complexity |
596
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(/C1N(C(C)C)C2C=CC=CC=2C=1C1C=CC(F)=CC=1)=C\[C@H](O)C[C@H](O)CC(=O)O.[Na]
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| InChi Key |
ZGGHKIMDNBDHJB-CALJPSDSSA-M
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| InChi Code |
InChI=1S/C24H26FNO4.Na/c1-15(2)26-21-6-4-3-5-20(21)24(16-7-9-17(25)10-8-16)22(26)12-11-18(27)13-19(28)14-23(29)30;/h3-12,15,18-19,27-28H,13-14H2,1-2H3,(H,29,30);/q;+1/p-1/b12-11+;
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| Chemical Name |
sodium;(E)-7-[3-(4-fluorophenyl)-1-propan-2-ylindol-2-yl]-3,5-dihydroxyhept-6-enoate
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| Synonyms |
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.77 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.77 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.77 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% propylene glycol, 5% Tween 80, 65% D5W:30 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3071 mL | 11.5354 mL | 23.0707 mL | |
| 5 mM | 0.4614 mL | 2.3071 mL | 4.6141 mL | |
| 10 mM | 0.2307 mL | 1.1535 mL | 2.3071 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01551173 | Completed Has Results | Drug: Fluvastatin sodium | Lipid Metabolism Disorders | Novartis Pharmaceuticals | January 2012 | Phase 4 |
| NCT03189511 | Completed | Drug: Fluvastatin | Adipose Tissue, Brown Insulin Resistance |
University of Zurich | May 31, 2017 | Phase 4 |
| NCT00674297 | Completed Has Results | Drug: Fluvastatin | Antiphospholipid Syndrome | Hospital for Special Surgery, New York | May 2008 | Phase 2 |
| NCT00664742 | Completed Has Results | Drug: Fluvastatin XL® | Metabolic Syndrome | Novartis | September 2006 | Phase 4 |
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