Home Metabolism HMG-CoA Reductase inhibitor Fluvastatin Sodium For research use only.

Fluvastatin Sodium

Synonyms: XU-62-320 Sodium

Fluvastatin Sodium inhibits HMG-CoA reductase activity with IC50 of 8 nM in a cell-free assay.

Fluvastatin Sodium Chemical Structure

Fluvastatin Sodium Chemical Structure

CAS No. 93957-55-2

Purity & Quality Control

Fluvastatin Sodium Related Products

Signaling Pathway

HMG-CoA Reductase Signaling Pathways

HMG-CoA Reductase Signaling Pathway

Biological Activity

Description Fluvastatin Sodium inhibits HMG-CoA reductase activity with IC50 of 8 nM in a cell-free assay.
Features The order of magnitude of inhibition of each drug on the peroxidation was butylated hydroxytoluene > fluvastatin ≥ probucol ≥ pravastatin.
Targets
HMG-CoA reductase [1]
(Cell-free assay)
8 nM
In vitro
In vitro

Fluvastatin markedly inhibits the formation of thiobarbituric acid reactive substances in iron (II)-supported peroxidation of liposomes with IC50 of 12 μM. Fluvastatin ranging from 1 μM to 100 μM inhibits peroxyl radical-mediated peroxidation of liposomes induced by water-soluble and lipid-soluble radical generators, 2,2'-azobis (2-amidinopropane) dihydro-chloride and 2,2'-azobis (2,4-dimethylvaleronitrile), respectively. [2] Fluvastatin (4 mM) and its metabolites shows superoxide anion scavenging activity in the hypoxanthine-xanthine oxidase system and a strong scavenging effect on the hydroxyl radical produced from Fenton's reaction. Fluvastatin (8 μM) and its metabolites shows protective effects on DNA damage as potent as the reference antioxidants, ascorbic acid, trolox, and probucol in CHL/IU cells. [3] Fluvastatin (100 nM) shows a dose-dependent decrease in Ang II-activated superoxide anion formation in human aortic smooth muscle cells (hASMC). [4]
Experimental Result Images Methods Biomarkers Images PMID
Western blot YAP1 / TAZ / RHAMM p53 / p21 / Cyclin D1 / ATF3 / H3P / PARP / Cleaved PARP / γ-H2AX 29212185
Growth inhibition assay Cell viability 26199863
Immunofluorescence YAP1 29212185
In Vivo
In vivo

Fluvastatin (10 mg/kg/day) results in a decrease in serum lipids in rabbits feed a 1.5% cholesterol containing diet. Fluvastatin (10 mg/kg/day) significantly lowers the tissue ACE in the aortae in rabbits feed a 1.5% cholesterol containing diet. Fluvastatin (10 mg/kg/day) significantly reverses the suppression of ACh-induced relaxation in rabbits feed a 1.5% cholesterol containing diet. [5]
Animal Research Animal Models Male Japanese white rabbits
Dosages 10 mg/kg
Administration Diet
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02115074 Completed
Glioma
Centre Oscar Lambret|Anticancer Fund Belgium
 June 2014 Phase 1
NCT01524601 Completed
Disorder Related to Renal Transplantation|Hypercholesterolemia
University of Oslo School of Pharmacy|Oslo University Hospital
 February 2012 Phase 4
NCT00814606 Withdrawn
Hepatitis C|Hepatitis C Virus
University of Chicago
 February 2010 Phase 2
NCT00752843 Completed
Healthy Subjects
Corcept Therapeutics
 September 2008 Phase 1
NCT00674297 Completed
Antiphospholipid Syndrome
Hospital for Special Surgery New York|University of Texas
 May 2008 Phase 2
NCT00404287 Terminated
Aortic Valve Stenosis
AORTICA Group
 October 1 2006 Phase 4

Chemical Information & Solubility

Molecular Weight 433.45 Formula

C24H25FNNaO4
CAS No. 93957-55-2 SDF Download Fluvastatin Sodium SDF
Smiles CC(C)N1C2=CC=CC=C2C(=C1C=CC(CC(CC(=O)[O-])O)O)C3=CC=C(C=C3)F.[Na+]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 87 mg/mL ( (200.71 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 18 mg/mL

Ethanol : Insoluble


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In vivo
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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.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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