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  3. Simvastatin

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

For research use only. We do not sell to patients.

Simvastatin Chemical Structure

Simvastatin Chemical Structure

CAS No. : 79902-63-9

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Customer Review

Based on 41 publication(s) in Google Scholar

Other Forms of Simvastatin:

Top Publications Citing Use of Products

37 Publications Citing Use of MCE Simvastatin

WB
Cell Viability Assay

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

    Simvastatin pretreatment maintains the expression of KLF2 and its protective target genes
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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]

    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].

    MedChemExpress (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.
    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].

    MedChemExpress (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
    Molecular Weight

    418.57

    Formula

    C25H38O5

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CCC(C)(C)C(O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(O3)=O)[C@@]12[H])=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    Ethanol : 100 mg/mL (238.91 mM; Need ultrasonic)

    DMSO : ≥ 50 mg/mL (119.45 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.97 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (5.97 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (23.89 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 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
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    • 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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