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

Simvastatin (Synonyms: MK 733)

Cat. No.: HY-17502 Purity: 99.45%
Handling Instructions

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 26 publication(s) in Google Scholar

Other Forms of Simvastatin:

Top Publications Citing Use of Products

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

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

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

    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: Clin Res Hepatol Gastroenterol. 2019 Apr;43(2):171-178.

    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.
    • 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 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.
    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
    Molecular Weight

    418.57

    Formula

    C25H38O5

    CAS No.
    SMILES
    Shipping

    Room temperature in continental US; may vary elsewhere.

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

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

    DMSO : ≥ 50 mg/mL (119.45 mM)

    *"≥" 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
    10 mM 0.2389 mL 1.1945 mL 2.3891 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

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

    • 2.

      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

    • 3.

      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

    • 4.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    • 5.

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

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

    • 6.

      Add each solvent one by one:  10% EtOH    90% corn oil

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

    *All of the co-solvents are available by MCE.
    Purity & Documentation
    References
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