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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/GC376/HY-100721/50mg
商品详细Medchemexpress/GC376/HY-100721/50mg
Medchemexpress/GC376/HY-100721/50mg
Medchemexpress/GC376/HY-100721/50mg
商品编号： HY-100721
品牌： MedChemExp
市场价： ¥42000.00
美元价： 25200.00
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
电子邮箱： info@ebiomall.com
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商品介绍
GC376isa3CLproinhibitor;inhibitsthereplicationofvirusesTGEV,FIPVandPTVwithIC50valuesof0.15,0.2and0.15μM.
Description

GC376isa3CLproinhibitor;inhibitsthereplicationofvirusesTGEV,FIPVandPTVwithIC50valuesof0.15,0.2and0.15μM.

IC50&Target

IC50:0.15μM(TGEV),0.2μM(FIPV),0.15μM(PTV),0.15μM(229E),1.1μM(MHV),5.3μM(MNV-1),0.6μM(BCV)[1]

InVitro

GC376covalentlybindstoCys139,Cys147,andCys144ofNV3CLpro,PV3Cpro,andTGEV3CLpro,respectively.GC376issignificantlyeffectiveagainstcaliciviruses(NVandMNV-1),coronaviruses(TGEV,FIPV,MHV,229E,andBCV),andpicornaviruses(HRVs18,51,and68,EV71,andPTV),withnanomolarorlowmicromolarIC50s,exceptforFCVandHAV.Interestingly,FCVislesssensitivetoGC376,withIC50of35μM.GC376showsnoorweakeffectivenessagainstthereplicationofHAVincells[1].ProteasesfromNV,MD145orMNV-1areinhibitedbyGC376withasimilarpotency.TheIC50valuesofGC376against3CLprofromNV,MD145,andMNV-1arecomparableamongtestedviruses[2].GC376effectivelyinhibitsthereplicationofNPI52-resistantvirusesincellcultureaswild-typeviruses,indicatingthatthemutationdoesnotconfercross-resistancetoGC376[3].

InVivo

GC376exhibitsfavorablebioavailABIlityandsafetyincats.GC376israpidlyabsorbedafters.c.admiNISTrationandthepeakplasmalevelisreachedwithin2hrafterinjection.Themeanplasmadrugconcentrationsremainsabovethe50%effectiveconcentration(EC50)valueofthealdehydeformofGC376(8ng/mL)for18hrspostinjection.Virusinfectedcatsshowsimprovementinattitudeandresolutionoffever.Theprofoundabsolutelymphopeniaobservedinallcatspriortoantiviraltreatmentalsoreturnstonormalbeforethenextbloodtestingoneweeklater[3].

References

  • [1].KimY,etal.Broad-spectrumantiviralsagainst3Cor3C-likeproteasesofpicornaviruses,noroviruses,andcoronaviruses.JVirol.2012Nov;86(21):11754-62.

    [2].TakahashiD,etal.Structuralandinhibitorstudiesofnorovirus3C-likeproteases.VirusRes.2013Dec26;178(2):437-44.

    [3].YunjeongKim,etal.ReversaloftheProgressionofFatalCoronavirusInfectioninCatsbyaBroad-SpectrumCoronavirusProteaseInhibitor.PLoSPathog.2016Mar30;12(3):e1005531.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM1.9703mL9.8516mL19.7033mL
5mM0.3941mL1.9703mL3.9407mL
10mM0.1970mL0.9852mL1.9703mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
KinaseAssay
[2]

Thestocksolution(10mM)ofGC376ispreparedinDMSOandfurtherdilutedinassaybuffer.ThefinalconcentrationsofDMSOintheassaydidnotexceed1.5%(vol/vol).The3CLprofromNV,MD145orMNV-1areincubatedwithvariousconcentrations(0.01to50µM)ofGC376in25µLofassaybufferfor30minat37°C.Followingincubation,25µLofassaybuffercontainingsubstrateisadded,andthemixturesareincubatedina96-wellblackplateat37°Cfor60min.Thefluorescencesignalsaredetectedusinganexcitationandemissionwavelengthof490and520nmonafluorescencemicroplatereader.TheRFUarecalculatedforeachwell,andthedose-dependentFRETinhibitioncurvesarefittedwithvariableslope(fourparameters)usingGraphPadPrismsoftwareinordertodeterminetheIC50valuesofGC376[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].KimY,etal.Broad-spectrumantiviralsagainst3Cor3C-likeproteasesofpicornaviruses,noroviruses,andcoronaviruses.JVirol.2012Nov;86(21):11754-62.

    [2].TakahashiD,etal.Structuralandinhibitorstudiesofnorovirus3C-likeproteases.VirusRes.2013Dec26;178(2):437-44.

    [3].YunjeongKim,etal.ReversaloftheProgressionofFatalCoronavirusInfectioninCatsbyaBroad-SpectrumCoronavirusProteaseInhibitor.PLoSPathog.2016Mar30;12(3):e1005531.

MolecularWeight

507.53

Formula

C₂₁H₃₀N₃NaO₈S

CASNo.

1416992-39-6

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO;InVivo:GC376isdissolvedin10%ethanoland90%PEG-400.

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

Purity:99.96%