Medchemexpress/PSI-7977（同义词：GS 7977；索福斯布韦）/HY-15005/50mg-免疫在线蚂蚁淘旗下平台

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商品详细Medchemexpress/PSI-7977（同义词：GS 7977；索福斯布韦）/HY-15005/50mg

Medchemexpress/PSI-7977（同义词：GS 7977；索福斯布韦）/HY-15005/50mg

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)

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

立即询价

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

ConcentrationVolumeMass	1mg	5mg	10mg

1mM	1.8888mL	9.4438mL	18.8875mL
5mM	0.3778mL	1.8888mL	3.7775mL
10mM	0.1889mL	0.9444mL	1.8888mL

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°C	3years
	4°C	2years
Insolvent	-80°C	6months
	-20°C	1month

Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

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

Purity:99.95%

SelectBatch: