Fluvastatin Sodium

製品コードS1909 バッチS190904

印刷

化学情報

Chemical Structure Synonyms XU-62-320 Sodium Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C24H25FNNaO4
分子量 433.45 CAS No. 93957-55-2
Solubility (25°C)* 体外 DMSO 87 mg/mL (200.71 mM)
Water 18 mg/mL (41.52 mM)
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
30%propylene glycol 5%Tween80 65%D5W
30.0mg/ml Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Fluvastatin Sodium inhibits HMG-CoA reductase activity with IC50 of 8 nM in a cell-free assay.
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]
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]
特徴 The order of magnitude of inhibition of each drug on the peroxidation was butylated hydroxytoluene > fluvastatin ≥ probucol ≥ pravastatin.

プロトコル(参考用のみ)

キナーゼアッセイ HMG-CoA reductase activity
The total volume of each assay is 95 μL and the reaction mixture contained 10 μL of the inhibiting compound to be tested and 85 μL of the incubating buffer containing 2 mg/mL liver microsomes, 0.1 M KH2P04, pH 7.2, 5.7 mM dithiothreitol, 10 mM glucose-6-phosphate, 2 U/mL glucose-6-phosphate dehydrogenase, 1 mM NADP, 10 μM miconazole. Control experiments are done without NADPH generating system. All samples are incubated 10 min at 37℃ before addition of 5 μL of substrate (unlabelled and 14C-HMG-3-hydroxy-3-methyl glutaryl CoA, final concentration 50 μM, 2.5 nCi/nmole). After 30 min at 37℃, the reaction is stopped by adding 27 μL 1N HCl and 20 μL of unlabelled mevalonolactone (200 μg/assay). The conversion of mevalonic acid to lactone is performed at room temperature for 60 min.
動物実験 動物モデル Male Japanese white rabbits
投薬量 10 mg/kg
投与方法 Diet

カスタマーフィードバック

Data from [Nat Genet, 2013, 45(9), 1013-20]

Data from [Nat Genet, 2013, 45(9), 1013-20]

Data from [Data independently produced by Biomark Res, 2013, 1(1), 33]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Combinatorial treatment with statins and niclosamide prevents CRC dissemination by unhinging the MACC1-β-catenin-S100A4 axis of metastasis [ Oncogene, 2022, 41(39):4446-4458] PubMed: 36008464
Deciphering COVID-19 host transcriptomic complexity and variations for therapeutic discovery against new variants [ iScience, 2022, 25(10):105068] PubMed: 36093376
Gene signature associated with resistance to fluvastatin chemoprevention for breast cancer [ BMC Cancer, 2022, 22(1):282] PubMed: 35296281
In situ assessment of statins' effect on autophagic activity in zebrafish larvae cardiomyocytes [ Front Cardiovasc Med, 2022, 9:921829] PubMed: 36465443
Ultra-fast proteomics with Scanning SWATH [ Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4] PubMed: 33767396
Intracellular cholesterol pools regulate oncogenic signaling and epigenetic circuitries in Early T-cell Precursor Acute Lymphoblastic Leukemia [ Cancer Discov, 2021, candisc.0551.2021] PubMed: 34711640
Computational analysis of cholangiocarcinoma phosphoproteomes identifies patient-specific drug targets [ Cancer Res, 2021, canres.0955.2021] PubMed: 34551960
Statin Drugs Plus Th1 Cytokines Potentiate Apoptosis and Ras Delocalization in Human Breast Cancer Lines and Combine With Dendritic Cell-Based Immunotherapy to Suppress Tumor Growth in a Mouse Model of HER-2 pos Disease [ Vaccines (Basel), 2020, 6;8(1):72] PubMed: 32041347
Delineation of cell death mechanisms induced by synergistic effects of statins and erlotinib in non-small cell lung cancer cell (NSCLC) lines. [ Sci Rep, 2020, 10(1):959] PubMed: 31969600
Strain-Dependent Variability of Early Discovery Small Molecule Pharmacokinetics in Mice: Does Strain Matter? [ Drug Metab Dispos, 2020, 48(8):613-621] PubMed: 32474442

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。