Simvastatin

Catalog No.S1792 Synonyms: MK-0733

Simvastatin  Chemical Structure

Molecular Weight(MW): 418.57

Simvastatin is a competitive inhibitor of HMG-CoA reductase with Ki of 0.1-0.2 nM in cell-free assays.

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Cited by 16 Publications

6 Customer Reviews

  • Statin-Related Inhibition of Dehydroepiandrosterone Sulfate (DHEAS) Uptake by SLCO2B1 in Prostate Cancer (PC) Cells. B, Uptake of DHEAS in PC cells with 2.5 µM DHEAS and different concentrations of statins when incubated for 60 minutes. Statistical analysis was performed by comparing each condition with the DHEAS 2.5 µM and no statin state except when indicated. C, Uptake of DHEAS in PC cells before (scrambled short hairpin RNA) and after (short hairpin RNA 2B1) SLCO2B1 is knocked down when incubated with 2.5 μM DHEAS and 100 μM atorvastatin for 10 and 60 minutes. Statistical analysis was performed by comparing each condition with scrambled short hairpin RNA after 10 minutes with DHEAS except when indicated. P = .02 for the comparison between scrambled short hairpin RNA with 10 vs 60 minutes of DHEAS incubation for LNCaP and .01 for 22RV1. Other P values are indicated in the figure. Bars indicate means and error bars indicate standard deviation.

    JAMA Oncol, 2015, 1(4):495-504. . Simvastatin purchased from Selleck.

  • Pharmacological inhibition of HMGR by simvastatin (250 nM) for 72 h, atorvastatin (10 μM) for 48 h or pitavastatin (1 μM) for 72 h. ***P<0.001; **P<0.01. Error bars = Mean ± SEM (n=3).

    Haematologica, 2018, doi: 10.3324/haematol.2018.204701. Simvastatin purchased from Selleck.

  • Representative images of p-Akt and p-GSK-3β expressions by western blot in the subgranular zone (SGZ) of the hippocampus.

    Cell Physiol Biochem, 2018, 46(2):618-632. Simvastatin purchased from Selleck.

  • HCMECs were incubated with simvastatin at a range of concentrations for 6 hr. Intracellular signaling responses were assessed by Western blotting for phosphorylation of ERK5 and ERK1/2 using phospho-specific antibodies. Unprenylation of Rap1A was measured as a control for simvastatin activity. Total protein was measured for ERK5, ERK1/2, and Rap1.

    J Cell Physiol, 2018, 233(1):186-200. Simvastatin purchased from Selleck.

  • Simvastatin obstructed autophagic flux induced by SAHA in MDA-MB-231. MDA-MB-231 cells that stable expressing (A) tfLC3 or (B) mRFP-LC3 were analyzed by confocal microscopy. MDA-MB-231 cells were treated with SAHA (1 μmol/l) and/or Simvastatin (1 μmol/l) for 16 h. Representative fluorescence images are shown.

    Eur J Pharmacol, 2018, 813:161-171. Simvastatin purchased from Selleck.

  • Graph showing retention of 99mTc-RGD measured by longitudinal SPECT imaging (~30 MBq, acquired from 70-90 mins post injection under isoflurane anaesthesia). Retention was significantly higher in the simvastatin treated ischemic limb compared to the vehicle treated ischemic limb on Days 3 and 8 post ligation (n=7 (n=3 blocked), *P<0.05, **P<0.01, 1-way ANOVA with post hoc Tuckey’s test, data shown as %ID/g ± SEM).

    Nucl Med Biol, 2017, 46:25-31. Simvastatin purchased from Selleck.

Purity & Quality Control

Choose Selective HMG-CoA Reductase Inhibitors

Biological Activity

Description Simvastatin is a competitive inhibitor of HMG-CoA reductase with Ki of 0.1-0.2 nM in cell-free assays.
Targets
HMG-CoA reductase [1]
(Cell-free assay)
0.1-0.2 nM(Ki)
In vitro

Prior to use in cell assays, Simvastatin needs to be activated by NaOH in EtOH treatment. Simvastatin inhibits cholesterol synthesis in mouse L-M cell (fibroblast), rat H4II E cell (liver), and human Hep G2 cell (liver) with IC50 of 19.3 nM, 13.3 nM and 15.6 nM, respectively. [1] Simvastatin treatment leads to a dose-dependent increase in serine 473 phosphorylation of Akt within 30 minutes, with maximal phosphorylation occurring at 1.0 µM. 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 displays anti-inflammatory effects in vitro. Simvastatin (10 μM) 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. Simvastatin (10 μM) suppresses cell-mediated macrophage TNF-γ release induced via cognate interactions by ~30%. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
rat liver hepatocytes MnLiSpVv[3Srb36gZZN{[Xl? NEDhRXE1KGh? MVLJcohq[mm2aX;uJI9nKGOqb3zld5Rmem:uIIP5cpRp\XOrczDpckBz[XRibHn2[ZIhcGWyYYTvZ5l1\XNiYX\0[ZIhPCCqcoOsJGlEPTB;MT6zJI5O NVH2WpRGOTd3NkC3PFg>
rat L6 cells NUfrTVI3TnWwY4Tpc44h[XO|YYm= Mmi1TY5pcWKrdHnvckBw\iClaH;s[ZN1\XKxbDDzfY51cGW|aYOgbY4hemG2IFy2JINmdGy|IHHzd4V{e2WmIHHzJIlv[2:{cH;yZZRqd25ib3[gX|E1S12jY3X0ZZRmKGmwdH:gZ4hwdGW|dHXyc4wtKEmFNUC9NE4xOjdizszN MoPFNVg1OTJ|MUe=
HepG2 cells NHTVOHZHfW6ldHnvckBie3OjeR?= NHzDbHBKdiC4aYTyc{BqdmirYnn0c5J6KGGldHn2bZR6KHejczDleoFtfWG2ZXSgc44h[2ixbHXzeIVzd2xiYnnvd5lvfGinc3nzJIlvKEincFeyJINmdGy|LDDJR|UxRTBwMESg{txO NXTscZk3OTR5NEGyOVg>
HEK293 cells MU\GeY5kfGmxbjDhd5NigQ>? NGLXbZJKdmirYnn0bY9vKG:oIF;BWHAySjFiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{KHW|aX7nJIV{fHKjZHnvcE0yP2KndHGt[4x2[3W{b37p[IUhe3Wkc4TyZZRmNCCLQ{WwQVQvPCEQvF2= MViyNlU5Pzl6Nh?=
human A549 cells MkjhR5l1d3SxeHnjxsBie3OjeR?= M3fCT|czKGh? NUnEVG9uS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVE3NjNizszN NFjJXlEzOzV5MEW0Ni=>
human HS68 cells M1H2NWN6fG:2b4jpZ:Kh[XO|YYm= M2r4SWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhUPjhiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2yOk41KM7:TR?= M3G3OFI{PTdyNUSy
mouse MEF cells M2fLTWN6fG:2b4jpZ:Kh[XO|YYm= MX3DfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDNSWYh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1|Nj63JO69VQ>? NWDwNJdQOjN3N{C1OFI>
RASMC cells MYjGeY5kfGmxbjDhd5NigQ>? NW[0TGVTOiEQvF2= Ml3kO|IhcA>? MnvLTY5pcWKrdHnvckBw\iC{YYSgSpRie2ViaX6gVmFUVUNiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJHJieyCycnXufYxifGmxbjDheEAzKHWPIHHmeIVzKDd{IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= NH25SlIzOThyMkm0Oi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Nrf2; 

PubMed: 27323826     


A. HCT116 cells were treated with 5 μM and 10 μM of simvastatin for 24 h. Nuclear fractions and cytoplasmic fractions were respectively analyzed by Western blotting for the detection of Nrf2 nuclear translocation Simvastatin increases the nuclear accumulation of Nrf2 in a dose-dependent manner. C. HT-29 cells were treated with the indicated concentrations of simvastatin for 24 h. Nuclear fractions and cytoplasmic fractions were respectively analyzed by Western blotting for the detection of Nrf2 nuclear translocation. Simvastatin increased the nuclear accumulation of Nrf2 in a dose-dependent manner. 

p-RB / Cyclin D1 / p21 / p27 / PCNA / CDC45 ; 

PubMed: 28300827     


Hep3B cells were treated with Simvastatin (5 or 10 μM) or Atorvastatin (20 or 40 μM) for 24 or 72 h, and cell extracts were analyzed by immunoblotting. The expression of MCM7, RB, p-RB, cyclin D1, PCNA and CDC45 were reduced and the expressions of p21 and p27 were increased.

AMPK / p-AMPK / P70S6 / p-P70S6 / LC3 / Atg7 ; 

PubMed: 28300827     


Hep3B cells were treated with 5 or 10 μM Simvastatin for 24 or 72 h, and then cell extracts were analyzed by immunoblotting with AMPK cell signaling or cell autophagy-related antibodies. 

Bcl-2 / PARP / Caspase-3 / Cleaved Caspase-3 ; 

PubMed: 28300827     


U2OS/SaOS2 and SiHa/C33A were treated with Simvastatin (2.5 or 5 μM) for 24 or 72 h, and then cell extracts were analyzed by immunoblotting with apoptosis-related antibodies

HMGCR ; 

PubMed: 26503475     


The effect of simvastatin on its target, HMGCR, was examined by Western blot analysis. Simvastatin treatment resulted in a dose-dependent decrease in expression of HMGCR protein in both cell lines.

27323826 28300827 26503475
Immunofluorescence
Nrf2; 

PubMed: 27323826     


B. HCT116 cells were treated with 10 μM simvastatin for 24 h. After treatment, cell was fixed and labeled with an anti-Nrf2 antibody, followed by a fluorescein isothiocyanate (FITC)-conjugated secondary antibody. The nuclei were visualized by DAPI staining. Simvastatin for 24 h increased the nuclear accumulation of Nrf2 protein from the cytoplasm to the nucleus by immunocytochemical analysis. D. HT-29 cells were treated with 10 μM simvastatin for 24 h. After treatment, cells were fixed and labeled with an anti-Nrf2 antibody, followed by an FITC-conjugated secondary antibody. The nuclei were visualized by DAPI staining. Simvastatin for 24 h increased the nuclear accumulation of Nrf2 protein from the cytoplasm to the nucleus by immunocytochemical analysis. The data represent three independent experiments. SV, simvastatin.

LC3A/B; 

PubMed: 28300827     


Hep3B cells were treated with serum starvation or 5 μM Simvastatin for 72 h. Cell monolayers were fixed and stained with LC3A/B, and immunofluorescence images were presented (Scale bars, 10 μm).

27323826 28300827
Growth inhibition assay
Cell viability; 

PubMed: 26503475     


Hey and SKOV3 cells were cultured for 24 h and then treated with varying concentrations of simvastatin in 96 well plates for 72 h. Cell proliferation was assessed by MTT assay.

26503475
In vivo Simvastatin orally administration inhibits the conversion of radiolabeled acetate to cholesterol with IC50 of 0.2 mg/kg. [1] Simvastatin (4 mg/day) orally administration for 13 weeks to rabbits fed an atherogenci cholesterol-rich diet, returns the cholesterol-induced increases in total cholesterol, LDL-cholesterol and HDL-cholesterol to normal level. [4] Simvastatin (6 mg/kg) produces an increase in LDL receptor-dependent binding and increases the number of hepatic LDL receptors in rabbits fed a diet containing 0.25% cholesterol. [5] Simvastatin influences inflammation independent of its effect on plasma cholesterol level. In cynomolgus monkeys consumed an atherogenic diet, Simvastatin (20 mg/kg/day) induces 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. [6]

Protocol

Solubility (25°C)

In vitro DMSO 83 mg/mL (198.29 mM)
Ethanol 83 mg/mL (198.29 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween80+ddH2O
For best results, use promptly after mixing.
10mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 418.57
Formula

C25H38O5

CAS No. 79902-63-9
Storage powder
in solvent
Synonyms MK-0733

Bio Calculators

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03571802 Not yet recruiting Drug: Simvastatin Obesity|Hyperlipidemias National University Hospital Singapore September 1 2018 Phase 4
NCT03387670 Recruiting Drug: Simvastatin|Drug: Placebo Secondary Progressive Multiple Sclerosis (SPMS) University College London|University of Edinburgh|Queen Mary University of London|London School of Hygiene and Tropical Medicine|University of Leeds|The Leeds Teaching Hospitals NHS Trust|Imperial College Healthcare NHS Trust March 28 2018 Phase 3
NCT03329118 Unknown status Drug: SHR3824 Simvastatin Type 2 Diabetes Jiangsu HengRui Medicine Co. Ltd. November 24 2017 Phase 1
NCT03660293 Completed Drug: Atorvastatin|Drug: Captopril|Drug: L-carnitine Diabetes Mellitus Type 1 Tanta University April 1 2017 Not Applicable

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    Can you please advise if Simvastatin has been tested effectively for in vivo use in mice? What solvent can be used to deliver Simvastatin in vivo?

  • Answer:

    This compound is an oral drug and a lot of studies report its use in mice. According to this paper (http://atvb.ahajournals.org/content/21/1/115.full), 0.5% Methyl-cellulose can be used as the vehicle.

  • Question 2:

    If any specific protocols exist for in vitro use, specifically any steps required to activate the compound?

  • Answer:

    This product is supplied in an inactive form and requires treatment with NaOH in EtOH followed by neutralization to pH 7.2 for activation. Please find the details from the following reference: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2739764/.

HMG-CoA Reductase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID