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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2 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.

    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 MoHsSpVv[3Srb36gZZN{[Xl? NUnGT|lHPCCq MXHJcohq[mm2aX;uJI9nKGOqb3zld5Rmem:uIIP5cpRp\XOrczDpckBz[XRibHn2[ZIhcGWyYYTvZ5l1\XNiYX\0[ZIhPCCqcoOsJGlEPTB;MT6zJI5O NEnRdWoyPzV4MEe4PC=>
rat L6 cells MmfKSpVv[3Srb36gZZN{[Xl? MYjJcohq[mm2aX;uJI9nKGOqb3zld5Rmem:uIIP5cpRp\XOrczDpckBz[XRiTE[gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kd3Kyb4LheIlwdiCxZjDbNVREZWGlZYTheIUhcW62bzDjbI9t\XO2ZYLvcEwhUUN3ME2wMlAzPyEQvF2= MVGxPFQyOjNzNx?=
HepG2 cells MoSySpVv[3Srb36gZZN{[Xl? MlT5TY4hfmm2cn:gbY5pcWKrdH;yfUBi[3Srdnn0fUB4[XNiZY\hcJVifGWmIH;uJINpd2ync4Tldo9tKGKrb4P5cpRp\XOrczDpckBJ\XCJMjDj[YxteyxiSVO1NF0xNjB2IN88US=> MkfrNVQ4PDF{NUi=
HEK293 cells M{X6UWZ2dmO2aX;uJIF{e2G7 NVzpZVZxUW6qaXLpeIlwdiCxZjDPRXRROUJzIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyC3c3nu[{Bme3S{YXTpc4wuOTekZYThMYdtfWO3cn;ubYRmKHO3YoP0doF1\SxiSVO1NF01NjRizszN NVm4b4tsOjJ3OEe5PFY>
human A549 cells NUPNPZhnS3m2b4TvfIlkyqCjc4PhfS=> NE[5fXA4OiCq M1fNbGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xOk4{KM7:TR?= MorBNlM2PzB3NEK=
human HS68 cells MW\DfZRwfG:6aXRCpIF{e2G7 NGThe3hEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJWzZ6IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NlYvPCEQvF2= NV21Xnk2OjN3N{C1OFI>
mouse MEF cells MnGxR5l1d3SxeHnjxsBie3OjeR?= MVnDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDNSWYh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1|Nj63JO69VQ>? NUjVbHV2OjN3N{C1OFI>
RASMC cells Mn;NSpVv[3Srb36gZZN{[Xl? M{H5XVIh|ryP MXm3NkBp NHXTZnpKdmirYnn0bY9vKG:oIILheEBHfGG|ZTDpckBTSVOPQzDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hWmG|IIDy[Y56dGG2aX;uJIF1KDJidV2gZYZ1\XJiN{KgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> MoHrNlE5ODJ7NE[=

... Click to View More Cell Line Experimental Data

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 individually and in order:
2% DMSO+30% PEG 300+5% Tween80+ddH2O
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
Synonyms MK-0733

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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The Serial Dilution Calculator Equation

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02447601 Completed Type 2 Diabetes Mellitus Jiangsu Hansoh Pharmaceutical Co., Ltd. March 30, 2015 Phase 1
NCT02533141 Not yet recruiting Healthy Medical University of Vienna May 2017 Phase 4
NCT02968810 Not yet recruiting Cirrhosis National Cancer Institute (NCI) February 2017 Phase 2
NCT02713945 Not yet recruiting Noonan Syndrome University Hospital, Toulouse December 2016 Phase 3
NCT02946424 Not yet recruiting Spinal Cord Injuries|Osteoporosis Craig Hospital November 2016 Phase 2
NCT02971410 Not yet recruiting Recurrent Plasma Cell Myeloma|Refractory Plasma Cell Myeloma Wake Forest University Health Sciences|National Cancer Institute (NCI) November 2016 --

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

If you have any other enquiries, please leave a message.

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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