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

Simvastatin  (Synonyms: 辛伐他汀; MK 733)

目录号: HY-17502 纯度: 99.56%
COA 产品使用指南

Simvastatin (MK 77333) 是一种具有口服活性的 HMG-CoA 还原酶 (HMGCR) 竞争性抑制剂, Ki 为 0.2 nM。Simvastatin 可减少胆固醇的合成,降低血液中的胆固醇水平。Simvastatin 对癌细胞表现出抗增殖活性,并能诱导细胞凋亡 (apoptosis)。

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Simvastatin Chemical Structure

Simvastatin Chemical Structure

CAS No. : 79902-63-9

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Other Forms of Simvastatin:

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 37 篇科研文献

WB
Cell Viability Assay

    Simvastatin purchased from MCE. Usage Cited in: Cancers (Basel). 2022, 14(22), 5601

    Simvastatin (0-40 µM; 48 h) inhibits growth of REC-1 and Z-138 cells with IC50 values of 4.97 µM and 3.78 µM, respectively.

    Simvastatin purchased from MCE. Usage Cited in: Clin Res Hepatol Gastroenterol. 2019 Apr;43(2):171-178.  [Abstract]

    Simvastatin pretreatment maintains the expression of KLF2 and its protective target genes (eNOS and TM). Westernblot analysis of KLF2, phosphorylation eNOS and total eNOS in liver tissue. β-actin is normalized as the loading control.

    Simvastatin purchased from MCE. Usage Cited in: J Biol Chem. 2018 Sep 14;293(37):14328-14341.  [Abstract]

    C4-2R cells are treated with Simvastatin, MDV3100 or combination of the two drugs at the indicated concentrations for 48 hours, followed by Immunoblotting (IB) against cleaved PARP.

    Simvastatin purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2017;2017:3861914.  [Abstract]

    Simvastatin pretreatment maintains the expression of KLF2 and its protective target genes
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.

    IC50 & Target

    Ki: 0.2 nM (HMG-CoA reductase)[1]

    体外研究
    (In Vitro)

    Simvastatin is an inactive drug precursor that has no drug activity itself and must be metabolized into its hydroxy acid form in the liver to function. In vitro experiments, it can be activated by sodium hydroxide (NaOH).
    Simvastatin suppresses cholesterol synthesis in mouse L-M cell, rat H4II E cell, and human Hep G2 cell with IC50s of 19.3 nM, 13.3 nM and 15.6 nM, respectively[1].
    Simvastatin causes a dose-dependent increase in serine 473 phosphorylation of Akt within 30 minutes, with maximal phosphorylation occurring at 1.0 µM[2].
    Simvastatin (1.0 μM) enhances phosphorylation of the endogenous Akt substrate endothelial nitric oxide synthase (eNOS), inhibits serum-free media undergo apoptosis and accelerates vascular structure formation[2].
    Simvastatin shows anti-inflammatory effects, reduces anti-CD3/anti-CD28 antibody-stimulated proliferation of PB-derived mononuclear cells and synovial fluid cells from rheumatoid arthritis blood, as well as IFN-γ release at 10 μM[3].
    Simvastatin (10 μM) also blocks cell-mediated macrophage TNF-γ release induced via cognate interactions by appr 30%[3].
    Simvastatin (5 μM) significantly reduces the expression of ABCA1 in astrocytes and neuroblastoma cells, the expression of apolipoprotein E in astrocytes, and increases cyclin-dependent kinase 5 and glycogen synthase kinase 3β expression in SK-N-SH cells[7].
    Simvastatin has the ability to inhibit exosome release[10].
    Simvastatin (32 and 64 μM; 24, 48, and 72 h) inhibits tumor cell growth, arrests in the G0/G1 phase[11].
    Simvastatin (32 and 64 μM; 48 h) induces apoptosis in HepG2 and Huh7 cells[11].

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

    Cell Proliferation Assay[11]

    Cell Line: HepG2 and Huh7 cells
    Concentration: 32 and 64 μM
    Incubation Time: 24, 48, and 72 hours
    Result: Inhibited tumor cell growth as compared to controls (ctrl, p<0.05).

    Apoptosis Analysis[11]

    Cell Line: HepG2 and Huh7 cells
    Concentration: 32 and 64 μM
    Incubation Time: 48 hours
    Result: Increased early apoptosis from 9.2% in non-treated ctrl cells to 18.2% (32 μM) and 19.8% (64 μM), respectively, increased late apoptosis from 35.0% in ctrl cells to 56.9% (32 μM) and 48.0% (64 μM), respectively, in HepG2 cells.

    Cell Cycle Analysis[11]

    Cell Line: HepG2 and Huh7 cells
    Concentration: 32 and 64 μM
    Incubation Time: 24, 48, and 72 hours
    Result: Exhibited downregulation of CDK1, CDK2, CDK4 and cyclins D1 and E as compared to ctrl tumor cells.
    体内研究
    (In Vivo)

    Simvastatin suppresses the conversion of radiolabeled acetate to cholesterol with an IC50 of 0.2 mg/kg via p.o. administration[1]. Simvastatin (4 mg/day, p.o. for 13 weeks) returns the cholesterol-induced increases in total cholesterol, LDL-cholesterol and HDL-cholesterol to normal level in rabbits fed an atherogenci cholesterol-rich diet[4].
    Simvastatin (6 mg/kg) increases LDL receptor-dependent binding and the number of hepatic LDL receptors in rabbits fed a diet containing 0.25% cholesterol[5].
    Simvastatin (20 mg/kg/day) causes a 1.3-fold less macrophage content in lesions, and 2-fold less vascular cell adhesion molecule-1, interleukin-1beta, and tissue factor expression, companied by a 2.1-fold increases in lesional smooth muscle cell and collagen content in cynomolgus monkeys fed an atherogenic diet[6].
    Simvastatin (oral gavage; 15 and 30 mg/kg; once daily; 14 d) treatment attenuats oxidative damage, TNF-a and IL-6 levels, and restores itochondrial enzyme complex activities[12].

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

    Animal Model: Male wistar rats with oxidative damage by Intrastriatal 6-OHDA administration[12]
    Dosage: 15 and 30 mg/kg
    Administration: Oral gavage; 15 and 30 mg/kg; once daily; 14 days
    Result: Attenuated oxidative damage (reduced MDA, nitrite levels and restoration of reduced GSH) , attenuated TNF-a and IL-6 levels, and restored itochondrial enzyme complex activities as compared to 6-OHDA group.
    Clinical Trial
    分子量

    418.57

    Formula

    C25H38O5

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    辛伐他汀;辛伐他丁

    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 1 year
    -20°C 6 months
    溶解性数据
    In Vitro: 

    Ethanol 中的溶解度 : 100 mg/mL (238.91 mM; 超声助溶)

    DMSO 中的溶解度 : ≥ 50 mg/mL (119.45 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 2.3891 mL 11.9454 mL 23.8909 mL
    5 mM 0.4778 mL 2.3891 mL 4.7782 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, 1 year; -20°C, 6 months。-80°C储存时,请在1个月内使用, -20°C储存时,请在6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

    In Vivo:

    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 (5.97 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 (5.97 mM); 悬浊液; 超声助溶

      此方案可获得 2.5 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      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。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):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。

    以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 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: 50% PEG300    50% Saline

      Solubility: 10 mg/mL (23.89 mM); 悬浊液; 超声助溶

    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
    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, 1 year; -20°C, 6 months。-80°C储存时,请在1个月内使用, -20°C储存时,请在6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 / Ethanol 1 mM 2.3891 mL 11.9454 mL 23.8909 mL 59.7272 mL
    5 mM 0.4778 mL 2.3891 mL 4.7782 mL 11.9454 mL
    10 mM 0.2389 mL 1.1945 mL 2.3891 mL 5.9727 mL
    15 mM 0.1593 mL 0.7964 mL 1.5927 mL 3.9818 mL
    20 mM 0.1195 mL 0.5973 mL 1.1945 mL 2.9864 mL
    25 mM 0.0956 mL 0.4778 mL 0.9556 mL 2.3891 mL
    30 mM 0.0796 mL 0.3982 mL 0.7964 mL 1.9909 mL
    40 mM 0.0597 mL 0.2986 mL 0.5973 mL 1.4932 mL
    50 mM 0.0478 mL 0.2389 mL 0.4778 mL 1.1945 mL
    60 mM 0.0398 mL 0.1991 mL 0.3982 mL 0.9955 mL
    80 mM 0.0299 mL 0.1493 mL 0.2986 mL 0.7466 mL
    100 mM 0.0239 mL 0.1195 mL 0.2389 mL 0.5973 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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    产品名称:
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    目录号:
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