Fluvastatin (XU 62-320 free ac

Fluvastatin  (Synonyms: 氟伐他汀; XU 62-320 free acid)

Fluvastatin (XU 62-320 free acid) 是第一个完全合成的，竞争性的 HMG-CoA 还原酶 抑制剂，IC₅₀ 为 8 nM。Fluvastatin 通过依赖 Nrf2 的抗氧化通路保护血管平滑肌细胞免受氧化应激。

美国medchemexpress（MCE)浙江省一级代理:杭州昊鑫生物科技股份有限公司
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生物活性    
Fluvastatin (XU 62-320 free acid) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1][2][3].

IC50 & Target    
IC50: 8 nM (HMG-CoA reductase)[1].

体外研究(In Vitro)    
Fluvastatin (XU 62-320 free acid) is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase (HMGCR), the enzyme that catalyzes the conversion of HMG-CoA to mevalonic acid, the rate-limiting step in cholesterol biosynthesis. Human hepatocellular carcinoma cell (HCC) studies indicate that Fluvastatin induces G2/M phase arrest. In the presence of Fluvastatin (XU 62320), HCC cells show a decrease of Bcl-2 and procaspase-9 expression, and an increase in Bax, cleaved caspase-3, and cytochrome c. Fluvastatin (XU 62320) is antilipemic and is used to reduce plasma cholesterol levels and prevent cardiovascular disease.

分子量    
411.47

Formula    
C24H26FNO4

CAS 号    
93957-54-1

中文名称    
氟伐他汀

运输条件    
Room temperature in continental US; may vary elsewhere.

储存方式    
Please store the product under the recommended conditions in the Certificate of Analysis.
 

参考文献

[1]. Araújo FA, Rocha MA, Capettini LS, et al. 3-Hydroxy-3-methylglutaryl coenzyme A reductase inhibitor (fluvastatin) decreases inflammatory angiogenesis in mice. APMIS. 2012 24. [Epub ahead of print]  [Content Brief] [2]. 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. [3]. Zhang W, Wu J, Zhou L, 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. [4]. Scripture CD, Pieper JA. Clinical pharmacokinetics of fluvastatin. Clin Pharmacokinet. 2001;40(4):263-81.  [Content Brief]