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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/Lovastatin（同义词：美维诺林）/HY-N0504/10mM*1mL二甲基亚砜
商品详细Medchemexpress/Lovastatin（同义词：美维诺林）/HY-N0504/10mM*1mL二甲基亚砜
Medchemexpress/Lovastatin（同义词：美维诺林）/HY-N0504/10mM*1mL二甲基亚砜
Medchemexpress/Lovastatin（同义词：美维诺林）/HY-N0504/10mM*1mL二甲基亚砜
商品编号： HY-N0504-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥1320.00
美元价： 792.00
产地： 美国(厂家直采)
公司：
产品分类： 小分子
公司分类： Small_molecule
联系Q Q： 3392242852
电话号码： 4000-520-616
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商品介绍
Lovastatin,aHMG-CoAreductaseinhibitor,isacholesterol-loweringdrug.
Description

Lovastatin,aHMG-CoAreductaseinhibitor,isacholesterol-loweringdrug.

InVitro

Lovastatinisaninactivelactoneprodrugthatmustbechemicallyorenzymaticallyconvertedtoitsdihydroxyopen-acidforminordertoelicitinhibitoryactivity.LovastatininitshydroxyacidformisanexceptionallypotentcompetitiveinhibitorofliverHMGCoAreductase[1].Lovastatin,otherthanitsanticholesterolproperty,hasdiverseapplicationsinthefieldofosteoporosis,neuro-degeneration,rheumatoidarthritis,antifungalsandalsoisreportedtoreduceproliferationoflungcancercells,breastcancer(MCF-7),livercancer(HepG2).LovastatintreatmentsshowsignificantdosedependentcytotoxiceffectonHeLacellswithIC50valueof160μg/mL.LovastatiniseffectivetoacceleratehydroxylrADIcalscavengingactivity(54.06%)atanIC50of3601μg/mL[2].

InVivo

Lovastatinisaninactivelactonethatishydrolyzedinthelivertoanactivef3-hydroxyacidform.ThisprincipalmetaboliteistheinhibitoroftheenzymeHMG-CoAreductase.TheKiis1nM.Lovastatinanditsβ-hydroxyacidmetabolitearehighlyboundtohumanplasmaproteins.Lovastatincrossestheblood-brainandplacentalbarriers[3].Lovastatinproducesaprofoundreductionofapolipoprotein-B-containinglipoproteins,especiallyLDLcholesteroland,toalesserextent,plasmatriglycerides,andasmallincreaseinHDLcholesterol[4].

ClinicalTrial
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References

  • [1].AlbertsAW,etal.Discovery,biochemistryandBIOLOGyoflovastatin.AmJCardiol.1988Nov11;62(15):10J-15J.

    [2].BhargaviS,etal.PurificationofLovastatinfromAspergillusterreus(KM017963)andEvaluationofitsAnticancerandAntioxidantProperties.AsianPacJCancerPrev.2016;17(8):3797-803.

    [3].FrishmanWH,etal.Lovastatin:anHMG-CoAreductaseinhibitorforloweringcholesterol.MedClinNorthAm.1989Mar;73(2):437-48.

    [4].TobertJA,etal.Lovastatinandbeyond:thehistoryoftheHMG-CoAreductaseinhibitors.NatRevDrugDiscov.2003Jul;2(7):517-26.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.4719mL12.3597mL24.7194mL
5mM0.4944mL2.4719mL4.9439mL
10mM0.2472mL1.2360mL2.4719mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[2]

Helacellsaretreatedwithlovastatin(0,5,10,20,40,80,160,320μg/mL)for24h.Cellstreatedwithculturemediumservesasanegativecontrol.cellviABIlityismeasuredusingtheMTTbasedcolorimetricassay[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].AlbertsAW,etal.Discovery,biochemistryandbiologyoflovastatin.AmJCardiol.1988Nov11;62(15):10J-15J.

    [2].BhargaviS,etal.PurificationofLovastatinfromAspergillusterreus(KM017963)andEvaluationofitsAnticancerandAntioxidantProperties.AsianPacJCancerPrev.2016;17(8):3797-803.

    [3].FrishmanWH,etal.Lovastatin:anHMG-CoAreductaseinhibitorforloweringcholesterol.MedClinNorthAm.1989Mar;73(2):437-48.

    [4].TobertJA,etal.Lovastatinandbeyond:thehistoryoftheHMG-CoAreductaseinhibitors.NatRevDrugDiscov.2003Jul;2(7):517-26.

MolecularWeight

404.54

Formula

C₂₄H₃₆O₅

CASNo.

75330-75-5

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥215mg/mL

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:99.47%