1. Metabolic Enzyme/Protease Autophagy Apoptosis
  2. HMG-CoA Reductase (HMGCR) Autophagy Ferroptosis
  3. Lovastatin

Lovastatin  (Synonyms: 洛伐他汀; Mevinolin)

目录号: HY-N0504 纯度: 99.64%
COA 产品使用指南

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

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Lovastatin Chemical Structure

Lovastatin Chemical Structure

CAS No. : 75330-75-5

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10 mM * 1 mL in DMSO ¥500
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50 mg ¥599
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100 mg ¥871
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200 mg ¥1200
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Customer Review

Other Forms of Lovastatin:

    Lovastatin purchased from MCE. Usage Cited in: Antiviral Res. 2022 Dec 15;209:105497.  [Abstract]

    Pretreatment with AY9944 (15, 30 µM), U18666A (5, 10 µM), lovastatin (5, 10 µM) and MβCD for 2 h can all significantly reduce the level of EV-A71 VP1 protein in HCT-8 cell.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol.

    IC50 & Target

    HMG-CoA reductase[1]

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    11.4 μM
    Compound: 1
    Cytotoxicity against human A549 cells after 72 hrs by MTT assay
    Cytotoxicity against human A549 cells after 72 hrs by MTT assay
    [PMID: 23570542]
    A549 IC50
    19.8 μM
    Compound: 1
    Inhibition of HMG-CoA reductase in human A549 cells after 5 mins by spectrophotometric analysis
    Inhibition of HMG-CoA reductase in human A549 cells after 5 mins by spectrophotometric analysis
    [PMID: 23570542]
    HepG2 IC50
    37 nM
    Compound: mevinolin (lactone) 2
    Concentration required to inhibit HMG-CoA reductase by 50% was determined in Hep G2 cell line
    Concentration required to inhibit HMG-CoA reductase by 50% was determined in Hep G2 cell line
    [PMID: 1527791]
    HepG2 IC50
    50 nM
    Compound: 1b (Mevinolin)
    Inhibition of cellular HMG-CoA reductase in cultures of human HEP G2 cells, determined by decreased incorporation of sodium [14C]acetate into cholesterol.
    Inhibition of cellular HMG-CoA reductase in cultures of human HEP G2 cells, determined by decreased incorporation of sodium [14C]acetate into cholesterol.
    [PMID: 2296036]
    HepG2 IC50
    8.3 μM
    Compound: Lovastatin
    Lipid lowering activity in human HepG2 cells assessed as decrease in oleic acid elicited lipid accumulation after 6 hrs by oil-red O staining method
    Lipid lowering activity in human HepG2 cells assessed as decrease in oleic acid elicited lipid accumulation after 6 hrs by oil-red O staining method
    [PMID: 26169125]
    HES IC50
    13 nM
    Compound: mevinolin (lactone) 2
    Concentration required to inhibit HMG-CoA reductase by 50% was determined in HES 9 cell line
    Concentration required to inhibit HMG-CoA reductase by 50% was determined in HES 9 cell line
    [PMID: 1527791]
    Hs68 IC50
    23.2 μM
    Compound: 1
    Cytotoxicity against human HS68 cells after 72 hrs by MTT assay
    Cytotoxicity against human HS68 cells after 72 hrs by MTT assay
    [PMID: 23570542]
    HT-29 IC50
    46.8 μM
    Compound: Lovastatin
    Growth inhibition of human HT29 cells after 96 hrs by MTS assay
    Growth inhibition of human HT29 cells after 96 hrs by MTS assay
    [PMID: 17472962]
    KB IC50
    15.6 μM
    Compound: 2
    Cytotoxicity against human KB cells by resazurin microplate assay
    Cytotoxicity against human KB cells by resazurin microplate assay
    [PMID: 27228159]
    LS180 IC50
    25.3 μM
    Compound: Lovastatin
    Growth inhibition of human LS180 cells after 96 hrs by MTS assay
    Growth inhibition of human LS180 cells after 96 hrs by MTS assay
    [PMID: 17472962]
    MCF7 IC50
    > 40 μM
    Compound: 1
    Cytotoxicity against human MCF7 cells assessed as growth inhibition after 24 to 48 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as growth inhibition after 24 to 48 hrs by MTT assay
    [PMID: 27756564]
    MDA-MB-231 IC50
    > 40 μM
    Compound: 1
    Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 24 to 48 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 24 to 48 hrs by MTT assay
    [PMID: 27756564]
    MEF IC50
    35 μM
    Compound: 1
    Cytotoxicity against mouse MEF cells after 72 hrs by MTT assay
    Cytotoxicity against mouse MEF cells after 72 hrs by MTT assay
    [PMID: 23570542]
    PC-3 IC50
    5.4 μM
    Compound: 1
    Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by SRB assay
    Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by SRB assay
    [PMID: 27756564]
    SW480 IC50
    7.1 μM
    Compound: Lovastatin
    Growth inhibition of human SW480 cells after 96 hrs by MTS assay
    Growth inhibition of human SW480 cells after 96 hrs by MTS assay
    [PMID: 17472962]
    T47D IC50
    > 40 μM
    Compound: 1
    Cytotoxicity against human T47D cells assessed as growth inhibition after 24 to 48 hrs by MTT assay
    Cytotoxicity against human T47D cells assessed as growth inhibition after 24 to 48 hrs by MTT assay
    [PMID: 27756564]
    THP-1 IC50
    8 μg/mL
    Compound: Lovastatin
    Inhibition of sICAM1/LFA1 interaction-mediated human THP1 cell adhesion after 1 hr by ELISA
    Inhibition of sICAM1/LFA1 interaction-mediated human THP1 cell adhesion after 1 hr by ELISA
    [PMID: 18672369]
    体外研究
    (In Vitro)

    Lovastatin (10 μM;72 hours) 有效降低 HepG2 细胞活力[2]
    Lovastatin (10 μM;48 hours) 诱导 HepG2 细胞凋亡[2]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Viability Assay[2]

    Cell Line: HepG2 cells
    Concentration: 10 μM
    Incubation Time: 72 hours
    Result: Efficiently reduced viability of HepG2 cells.
    体内研究
    (In Vivo)

    Lovastatin 是一种无活性内酯,在肝脏中水解为活性 f3-羟基酸形式。这种主要代谢物是 HMG-CoA 还原酶的抑制剂。Ki 为 1 nM。Lovastatin 及其 β-羟基酸代谢物与人血浆蛋白高度结合。Lovastatin 可穿过血脑屏障和胎盘屏障[3]。Lovastatin 可显著降低含载脂蛋白 B 的脂蛋白,尤其是 LDL 胆固醇,并在较小程度上降低血浆甘油三酯,并略微增加 HDL 胆固醇[4]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    分子量

    404.54

    Formula

    C24H36O5

    CAS 号
    性状

    固体

    颜色

    Off-white to light yellow

    中文名称

    洛伐他汀; 辛伐他汀EP杂质E

    结构分类
    初始来源

    aspergillus terreus

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : ≥ 100 mg/mL (247.19 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.4719 mL 12.3597 mL 24.7194 mL
    5 mM 0.4944 mL 2.4719 mL 4.9439 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.18 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.18 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.89%

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.4719 mL 12.3597 mL 24.7194 mL 61.7986 mL
    5 mM 0.4944 mL 2.4719 mL 4.9439 mL 12.3597 mL
    10 mM 0.2472 mL 1.2360 mL 2.4719 mL 6.1799 mL
    15 mM 0.1648 mL 0.8240 mL 1.6480 mL 4.1199 mL
    20 mM 0.1236 mL 0.6180 mL 1.2360 mL 3.0899 mL
    25 mM 0.0989 mL 0.4944 mL 0.9888 mL 2.4719 mL
    30 mM 0.0824 mL 0.4120 mL 0.8240 mL 2.0600 mL
    40 mM 0.0618 mL 0.3090 mL 0.6180 mL 1.5450 mL
    50 mM 0.0494 mL 0.2472 mL 0.4944 mL 1.2360 mL
    60 mM 0.0412 mL 0.2060 mL 0.4120 mL 1.0300 mL
    80 mM 0.0309 mL 0.1545 mL 0.3090 mL 0.7725 mL
    100 mM 0.0247 mL 0.1236 mL 0.2472 mL 0.6180 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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