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Fluvastatin Sodium HMG-CoA Reductase inhibitor

Cat.No.S1909

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

Batch: Purity: 99.99%
99.99

Solubility

In vitro
Batch:

DMSO : 87 mg/mL (200.71 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 18 mg/mL

Ethanol : Insoluble

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In vivo
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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.

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Chemical Information, Storage & Stability

Molecular Weight 433.45 Formula

C24H25FNNaO4

Storage (From the date of receipt)
CAS No. 93957-55-2 Download SDF Storage of Stock Solutions

Synonyms XU-62-320 Sodium SMILES CC(C)N1C2=CC=CC=C2C(=C1C=CC(CC(CC(=O)[O-])O)O)C3=CC=C(C=C3)F.[Na+]

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Mechanism of Action

Features
The order of magnitude of inhibition of each drug on the peroxidation was butylated hydroxytoluene > fluvastatin ≥ probucol ≥ pravastatin.
Targets/IC50/Ki
HMG-CoA reductase
(Cell-free assay)
8 nM
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. 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. Fluvastatin (100 nM) shows a dose-dependent decrease in Ang II-activated superoxide anion formation in human aortic smooth muscle cells (hASMC).

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.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/12374897/
  • [5] https://pubmed.ncbi.nlm.nih.gov/8937733/

Applications

Methods Biomarkers Images PMID
Western blot YAP1 / TAZ / RHAMM p53 / p21 / Cyclin D1 / ATF3 / H3P / PARP / Cleaved PARP / γ-H2AX
S1909-WB1
29212185
Growth inhibition assay Cell viability
S1909-viability1
26199863
Immunofluorescence YAP1
S1909-IF1
29212185

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-01-21)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06785727 NOT_YET_RECRUITING
Ischemic Stroke; Transient Ischemic Attack
Prof. dr. Nathalie van der Velde
2025-02-01 PHASE4
NCT06679036 RECRUITING
Advanced Unresectable or Metastatic Breast Cancer
Shandong Suncadia Medicine Co., Ltd.
2025-01-21 PHASE1; PHASE2
NCT06830954 NOT_YET_RECRUITING
Bioequivalence
Shenzhen Salubris Pharmaceuticals Co., Ltd.
2025-02 PHASE1
NCT06262685 UNKNOWN
Cardiovascular Diseases; Dyslipidemias; Statin Adverse Reaction; Pharmacogenic Myopathy
Instituto de Investigación Hospital Universitario La Paz
2024-03-04 PHASE4
NCT04285749 WITHDRAWN
Malignant Melanoma
Case Comprehensive Cancer Center
2020-11-06 EARLY_PHASE1
NCT03510884 COMPLETED
Hypercholesterolaemia
Sanofi
2018-05-31 PHASE3

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