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Fluvastatin Sodium Salt

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Chemical Structure| 93957-55-2 同义名 : 氟伐他汀钠 水合物 ;Fluvastatin sodium;XU 62-320
CAS号 : 93957-55-2
货号 : A109438
分子式 : C24H25FNNaO4
纯度 : 98%
分子量 : 433.448
MDL号 : MFCD00929076
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(115.35 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(115.35 mM)，配合低频超声助溶
动物实验配方：

PO 0.5% CMC-Na 40 mg/mL suspension

生物活性
描述 Fluvastatin sodium (XU 62320) is a first fully synthetic, competitive HMG-CoA reductase inhibitor. the statin (0.6 and 6 mg/kg/day) inhibited hemoglobin (Hb) content (51%) and vascular endothelial growth factor (VEGF) levels (71%) in the treated group compared with the control group. The inflammatory component, as assessed by N-acetyl-β-D-glucosaminidase activity and tumor necrosis factor-α (TNF-α) level was also decreased by the compound. In the treated group; the inhibition of the enzyme activity was 33% and the cytokine was 67% relative to the control.[4].Untreated Apolipoprotein E–deficient Control mice developed severe hypercholesterolemia and hypertriglyceridemia and had a significantly lower HDL cholesterol level (-70%) compared with the age-matched wild type mice.Compared with ApoE-/- mice, chronic fluvastatin treatment significantly decreased plasma total cholesterol (-53%) and HDL cholesterol levels (-61%) and normalized triglycerides[5]. Fluvastatin is extensively absorbed from the gastrointestinal tract. After absorption, it is nearly completely extracted and metabolised in the liver to 2 hydroxylated metabolites and an N-desisopropyl metabolite, which are excreted in the bile. Approximately 95% of a dose is recovered in the faeces, with 60% of a dose recovered as the 3 metabolites. The 6-hydroxy and N-desisopropyl fluvastatin metabolites are exclusively generated by cytochrome P450 (CYP) 2C9 and do not accumulate in the blood. CYP2C9, CYP3A4, CYP2C8 and CYP2D6 form the 5-hydroxy fluvastatin metabolite[6].
作用机制 Fluvastatin exerts cytoprotective effects against oxidative stress, inducing antioxidant genes through Nrf2/ARE in hCASMCs[3].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00256750 Kidney Transplantation ... 展开 >> Chronic Kidney Failure 收起 << Phase 3 Completed - -
NCT01563731 Stroke Transi... 展开 >>ent Ischemic Attack Hypertension 收起 << Phase 4 Recruiting November 2018 Russian Federation ... 展开 >> Almazov Federal Heart, Blood and Endocrinology Centre Recruiting Saint-Petersburg, Russian Federation, 197341 收起 <<
NCT01047501 Hypertriglyceridemia Phase 3 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.54mL

2.31mL

1.15mL

23.07mL

4.61mL

2.31mL
参考文献

[1]Kugi M, Matsunaga A, et al. Antioxidative effects of fluvastatin on superoxide anion activated by angiotensin II in human aortic smooth muscle cells. Cardiovasc Drugs Ther. 2002 May;16(3):203-7.

[2]Mitani H, Bandoh T, et al. Inhibitory effects of fluvastatin, a new HMG-CoA reductase inhibitor, on the increase in vascular ACE activity in cholesterol-fed rabbits. Br J Pharmacol. 1996 Nov;119(6):1269-75.

[3]Makabe S, Takahashi Y, Watanabe H, et al. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway. Atherosclerosis. 2010 Dec;213(2):377-84.

[4] Fernanda A Araújo,et al. 3-Hydroxy-3-methylglutaryl coenzyme A reductase inhibitor (fluvastatin) decreases inflammatory angiogenesis in mice. APMIS. 2013 May;121(5):422-30.

[5] Marianne Gervais,et al. Fluvastatin prevents renal dysfunction and vascular NO deficit in apolipoprotein E-deficient mice, Arterioscler Thromb Vasc Biol. 2003 Feb 1;23(2):183-9.

[6] Scripture CD, Pieper JA. Clinical pharmacokinetics of fluvastatin. Clin Pharmacokinet. 2001;40(4):263-81.