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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/Ledipasvir(Synonyms: GS-5885)/HY-15602/50mg
商品详细Medchemexpress/Ledipasvir(Synonyms: GS-5885)/HY-15602/50mg
Medchemexpress/Ledipasvir(Synonyms: GS-5885)/HY-15602/50mg
Medchemexpress/Ledipasvir(Synonyms: GS-5885)/HY-15602/50mg
商品编号： HY-15602-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥2120.00
美元价： 1272.00
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
LedipasvirisaninhibitorofthehepatitisCvirusNS5A,withEC50valuesof34pMagainstGT1aand4pMagainstGT1breplicon.

CustomerValidation

  • •ProcNatlAcadSciUSA.2017Feb21;114(8):1922-1927.
  • •IntJRADIatOncolBiolPhys.2016Nov15;96(4):867-876.
  • •AntimicrobAgentsChemother.2015Jun;59(6):3482-92.
  • •AntimicrobAgentsChemother.2015May;59(5):2496-507.
  • •AntimicrobAgentsChemother.2014Sep;58(9):5386-94.
  • •AntiviralRes.2017Mar;139:18-24.
  • •PLoSOne.2016Jul21;11(7):e0159511.
  • •NeurosciLett.2015Nov16;609:48-52.
  • •TransplInfectDis.2017Nov7.
  • •North-WestUniversity.2014.
Description

LedipasvirisaninhibitorofthehepatitisCvirusNS5A,withEC50valuesof34pMagainstGT1aand4pMagainstGT1breplicon.

IC50&Target

EC50:34pM(GT1a),4pM(GT1b)[1]

InVitro

LedipasvirhasGT1aand1bEC50valuesof31and4pM,respectively,andprotein-adjustedEC50valuesof210pM(GT1a)and27pM(GT1b)andtheintrinsicEC50of39is310fMforGT1aand40fMforGT1b.Ledipasvirishighlyprotein-boundbothinhumanserumandinthecell-culturemedium(containing10%BSA)oftherepliconassay[1].LedipasvirexhibitsanEC50valueof141nMagainsttheJFH/3a-NS5Areplicon[2].

InVivo

Ledipasvirisremarkablenotonlyonthebasisofitshighrepliconpotencybutalsoonthebasisofitslowclearance,goodbioavailABIlity,andlonghalf-livesinrat,dog,andmonkeyandlowpredictedclearanceinhuman.ThepharmacokineticsofLedipasvirismeasuredinratsanddogs.Ledipasvirshowsgoodhalf-lives(rat1.83±0.22hr,dog2.63±0.18hr)inplasma,lowsystemicclearance(CL),andmoderatevolumesofdistribution(Vss)thataregreaterthantotalbodywatervolume[1].

ClinicalTrial
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References

  • [1].LinkJO,etal.Discoveryofledipasvir(GS-5885):apotent,once-dailyoralNS5AinhibitorforthetreatmentofhepatitisCvirusinfection.JMedChem.2014Mar13;57(5):2033-46.

    [2].HernandezD,etal.NaturalprevalenceofNS5ApolymorphismsinsubjectsinfectedwithhepatitisCvirusgenotype3andtheireffectsontheantiviralactivityofNS5Ainhibitors.JClinVirol.2013May;57(1):13-8.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM1.1249mL5.6243mL11.2486mL
5mM0.2250mL1.1249mL2.2497mL
10mM0.1125mL0.5624mL1.1249mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
AnimalAdmiNISTration
[1]

Intravenous(IV)administrationisdosedviainfusionover30mininavehiclecontaining5%ethanol,20%PEG400,and75%water(pHadjustedto3.0withHCl)[1].
Oraldosingisadministeredbygavageinavehiclecontaining5%ethanol,45%PEG400,and50%of50mMcitratebuffer,pH3[1].

Rat,DogandMonkey[1]
Pharmacokineticstudiesareperformedinmalenaı̈veSprague-Dawley(SD)rats,non-naı̈vebeagledogs,andcynomolgusmonkeys(threeanimalsperdosingroute).Intravenous(IV)administrationisdosedviainfusionover30mininavehiclecontaining5%ethanol,20%PEG400,and75%water(pHadjustedto3.0withHCl).Oraldosingisadministeredbygavageinavehiclecontaining5%ethanol,45%PEG400,and50%of50mMcitratebuffer,pH3.Bloodsamplesarecollectedovera24hperiodpostdoseintoVacutainertubescontainingEDTA-K2.Plasmawasisolated,andtheconcentrationofthetestcompoundinplasmawasdeterminedwithLC/MS/MSafterproteinprecipitationwithacetonitrile.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].LinkJO,etal.Discoveryofledipasvir(GS-5885):apotent,once-dailyoralNS5AinhibitorforthetreatmentofhepatitisCvirusinfection.JMedChem.2014Mar13;57(5):2033-46.

    [2].HernandezD,etal.NaturalprevalenceofNS5ApolymorphismsinsubjectsinfectedwithhepatitisCvirusgenotype3andtheireffectsontheantiviralactivityofNS5Ainhibitors.JClinVirol.2013May;57(1):13-8.

MolecularWeight

889.0

Formula

C₄₉H₅₄F₂N₈O₆

CASNo.

1256388-51-8

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:>98.0%