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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/PSI-7977(Synonyms: GS 7977; sofosbuvir)/HY-15005/10mg
商品详细Medchemexpress/PSI-7977(Synonyms: GS 7977; sofosbuvir)/HY-15005/10mg
Medchemexpress/PSI-7977(Synonyms: GS 7977; sofosbuvir)/HY-15005/10mg
Medchemexpress/PSI-7977(Synonyms: GS 7977; sofosbuvir)/HY-15005/10mg
商品编号： HY-15005-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥1160.00
美元价： 696.00
产地： 美国(厂家直采)
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产品分类： 小分子
公司分类： Small_molecule
联系Q Q： 3392242852
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商品介绍
PSI-7977isanactiveinhibitorofHCVRNAreplicationintheHCVrepliconassay,demonstratespotentanti-hepatitisCvirus(HCV)activity.

CustomerValidation

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Description

PSI-7977isanactiveinhibitorofHCVRNAreplicationintheHCVrepliconassay,demonstratespotentanti-hepatitisCvirus(HCV)activity.

IC50&Target

EC50:92±5nM(HCV)[1]

InVitro

WhencathepsinA(CatA)isincubatedwithPSI-7977orPSI-7976for150min,~18-foldmorePSI-352707isformedwhenPSI-7977isthesubstratecomparedwithPSI-7976.Moreover,thecatalyticefficiencyforPSI-7977withCatAis~30-foldhigherthanthatforPSI-7976[1].ThegenotypecoverageofPSI-7977byusingGT1b(Con1)-,1a(H77)-,and2a(JFH-1)-derivedrepliconsandGT1bchimericrepliconscontainingtheNS5BregionfromtheJ6GT2aisolateandfromGT2bandGT3apatientisolatesisevaluated,PSI-7977inhibitsthereplicationoftheserepliconswithsimilarEC50s(between16and48nM),andisespeciallyactiveagainstthechimericrepliconcontainingtheJ6NS5B(EC50=4.7nM).PSI-7977inhibitscloneA(GT1b)wild-typeandS282TrepliconswithEC90valuesof0.42and7.8μM,respectively[2].InthecloneArepliconassay,PSI-7977producesanti-HCVactivitywithEC90values0.42μM[3].

ClinicalTrial
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References

  • [1].MurakamiE,etal.MechanismofactivationofPSI-7851anditsdiastereoisomerPSI-7977.JBiolChem.2010Nov5;285(45):34337-47.

    [2].LamAM,etal.GenotypeandsubtypeprofilingofPSI-7977asanucleotideinhibitorofhepatitisCvirus.AntimicrobAgentsChemother.2012Jun;56(6):3359-68.

    [3].SofiaMJ,etal.Discoveryofaβ-d-2"-deoxy-2"-α-fluoro-2"-β-C-methyluridinenucleotideprodrug(PSI-7977)forthetreatmentofhepatitisCvirus.JMedChem.2010Oct14;53(19):7202-18.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM1.8888mL9.4438mL18.8875mL
5mM0.3778mL1.8888mL3.7775mL
10mM0.1889mL0.9444mL1.8888mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[1]

PSI-7977isdissolvedinDMSOandstored,andthendilutedwithappropriatemediumbeforeuse[1].

CloneAcellsareseededintoT75flasksatabout5×106cells/flaskinDulbecco"smodifiedEagle"smedium(DMEM)containing100IU/mLPenicillin/100μg/mLstreptomycinand10%fetalbovineserum.Similarly,humanprimaryhepatocytesareseededincellplatingmediumintoT75flasksatabout5×106cells/flask.Afterovernightincubationtoallowthecellstoattach,cellsareincubatedwith50μMPSI-7851,PSI-7976,orPSI-7977infreshmediumforcloneAcellsorincellmaintenancemediumforprimaryhepatocytesforupto24hat37°Cina5%CO2atmosphere.ThesameproceduresareappliedwhenradiolabeledPSI-7851isusedinthestudyexceptthat1×106cellsperwellareseededintoa6-wellplate,andthecellsareincubatedwith5μM[3H]PSI-7851.Atselectedtimes,themediumisremoved,andthecelllayeriswashedwithcoldphosphate-bufferedsaline(PBS).Aftertrypsinization,cellsarecountedandcentrifugedat1,200rpmfor5min.ThecellpelletsaresUSPendedin1mLofcold60%methanolandincubatedovernightat−20°C.Thesamplesarecentrifugedat14,000rpmfor5min,andthesupernatantsarecollectedanddriedusingaSpeedVacconcentratorandstoredat−20°Cuntiltheyareanalyzedbyhighperformanceliquidchromatography(HPLC).Residuesaresuspendedin100μLofwater,and50-μLaliquotsareinjectedintoHPLC[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].MurakamiE,etal.MechanismofactivationofPSI-7851anditsdiastereoisomerPSI-7977.JBiolChem.2010Nov5;285(45):34337-47.

    [2].LamAM,etal.GenotypeandsubtypeprofilingofPSI-7977asanucleotideinhibitorofhepatitisCvirus.AntimicrobAgentsChemother.2012Jun;56(6):3359-68.

    [3].SofiaMJ,etal.Discoveryofaβ-d-2"-deoxy-2"-α-fluoro-2"-β-C-methyluridinenucleotideprodrug(PSI-7977)forthetreatmentofhepatitisCvirus.JMedChem.2010Oct14;53(19):7202-18.

MolecularWeight

529.45

Formula

C₂₂H₂₉FN₃O₉P

CASNo.

1190307-88-0

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

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

Purity:99.95%