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/ Lovastatin

洛伐他汀 /Lovastatin {[allProObj[0].p_purity_real_show]}

货号：A151986 同义名： Mevinolin;Monacolin K

Lovastatin是一种用于降低胆固醇的细胞渗透性 HMG-CoA 还原酶抑制剂。

Lovastatin 化学结构 CAS号：75330-75-5
Lovastatin 化学结构
CAS号：75330-75-5
Lovastatin 3D分子结构
CAS号：75330-75-5
Lovastatin 化学结构 CAS号：75330-75-5
Lovastatin 3D分子结构 CAS号：75330-75-5
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Lovastatin 纯度/质量文件 产品仅供科研

货号：A151986 标准纯度： {[allProObj[0].p_purity_real_show]}
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Lovastatin 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].

Lovastatin 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
human A549 cells Cytotoxic assay 72 h Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=11.4 μM 23570542

Lovastatin 动物研究

Dose Mice: 400 mg/kg[3] (p.o.) Nude: 1 mg/kg - 10 mg/kg[4] (p.o.)
Administration p.o.

Lovastatin 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 - -

Lovastatin 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.

Lovastatin 实验方案

计算器
存储液制备 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

Lovastatin 技术信息

CAS号75330-75-5
分子式C24H36O5
分子量 404.54
别名 Mevinolin;Monacolin K;Altoprev;Mevacor;NSC 633781;(+)-Mevinolin;MK-803
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature
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

Tags: Lovastatin | Mevinolin;Monacolin K;Altoprev;Mevacor;NSC 633781;(+)-Mevinolin;MK-803 | Cardiovascular System | Drug Standard | Reduce Blood Lipid | Inosine Monophosphate (IMP) Dehydrogenase Inhibitor | HMGCR | AmBeed-信号通路专用抑制剂 | Lovastatin 纯度/质量文件 | Lovastatin 生物活性 | Lovastatin 细胞研究 | Lovastatin 动物研究 | Lovastatin 临床数据 | Lovastatin 参考文献 | Lovastatin 实验方案 | Lovastatin 技术信息

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