产品说明书

Lovastatin

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Chemical Structure| 75330-75-5 同义名 : Mevinolin;Monacolin K;Altoprev;Mevacor;NSC 633781;(+)-Mevinolin;MK-803
CAS号 : 75330-75-5
货号 : A151986
分子式 : C24H36O5
纯度 : 98%
分子量 : 404.54
MDL号 : MFCD00072164
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(259.55 mM)，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
动物实验配方：

5% DMSO+40%PEG 300+ 5% Tween80 + 50% water 2.5 mg/mL

生物活性
描述 HMG-CoA reductase (HMGCR) is a rate-limiting enzyme in cholesterol synthesis. Lovastatin is a potent inhibitor of HMGCR with an Ki value of 0.6 nM[3]. In human myeloid leukemia KBM-5 cells, treatment with 5 – 50 μM lovastatin for 12 hours effectively inhibited TNF-induced NF-κB activation at a dose-dependent manner. Incubation of KBM-5 cells with 5 μM lovastatin for 24 hours enhanced cytotoxicity induced by chemotherapeutic agents (i.e. paclitaxel, doxorubicin, and 5-fluorouracil). The same treatment also augmented chemotherapeutic agents-induced apoptotic effects in KBM-5 cells[4]. In rat primary astrocytes, 8h preincubation with 10 μM lovastatin led to 90% inhibition of LPS-induced NO production. Pretreatment with 5 or 10 μM lovastatin for 8 hours also significantly suppressed LPS-mediated induction of iNOS mRNA and protein. A combination of lovastatin (2 μM) and sodium phenylacetate (2 nM) almost completely inhibited LPS-induced NO production and iNOS expression. The addition of 10 μM lovastatin to rat primary astrocytes inhibited cholesterol synthesis by 73% and reduced NO production induced by different combinations of LPS and cytokines. Lovastatin (10 μM) also showed potent inhibitory effect on LPS-induced production of NO, TNF-a, IL-1b, and IL-6 in rat primary microglia and macrophages[5]. In nf1+/− mice, daily injection with lovastatin (10 mg/kg) for 4 days decreased the level of phosphorylated p44/42 MAPK compared to wild-type controls. Lovastatin treatment also resulted in an improvement in sensory gating deficits and long-term potentiation in nf1+/− mice[6].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
HEP G2 cells Function assay Inhibition of cellular HMG-CoA reductase in cultures of hepatic cells (HEP G2, a human hepatoma cell line), IC50=5e-05 μM 2153213
HEP G2 cells Function assay Tested for inhibition of cholesterol biosynthesis in HEP G2 cells, IC50=0.029 μM 7932551
HES 9 cell line Function assay Concentration required to inhibit HMG-CoA reductase by 50% was determined in HES 9 cell line, IC50=0.013 μM 1527791
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
NCT01047683 Hypertriglyceridemia Phase 3 Completed - -
NCT00256750 Kidney Transplantation ... 展开 >> Chronic Kidney Failure 收起 << Phase 3 Completed - -
NCT01047501 Hypertriglyceridemia Phase 3 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.47mL

0.49mL

0.25mL

12.36mL

2.47mL

1.24mL

24.72mL

4.94mL

2.47mL
参考文献

[1]85(14):5264-8.

[2]75(4):907-13.

[3]Singer II, Scott S, Kazazis DM, Huff JW. Lovastatin, an inhibitor of cholesterol synthesis, induces hydroxymethylglutaryl-coenzyme A reductase directly on membranes of expanded smooth endoplasmic reticulum in rat hepatocytes. Proc Natl Acad Sci U S A. 1988 Jul;85(14):5264-8.

[4]Ahn KS, Sethi G, Aggarwal BB. Reversal of chemoresistance and enhancement of apoptosis by statins through down-regulation of the NF-kappaB pathway. Biochem Pharmacol. 2008 Feb 15;75(4):907-13.