Medchemexpress/奥司他韦酸（同义词：GS 4071；Ro 64-0802；羧酸奥司他韦）/HY-13318/5mg-免疫在线蚂蚁淘旗下平台

当前位置：首页 > 产品中心 > Small_molecule > Medchemexpress/奥司他韦酸（同义词：GS 4071；Ro 64-0802；羧酸奥司他韦）/HY-13318/5mg

商品详细Medchemexpress/奥司他韦酸（同义词：GS 4071；Ro 64-0802；羧酸奥司他韦）/HY-13318/5mg

Medchemexpress/奥司他韦酸（同义词：GS 4071；Ro 64-0802；羧酸奥司他韦）/HY-13318/5mg

商品编号： HY-13318-10mM*1mLinDMSO

品牌： MedChemExp

市场价： ¥1720.00

美元价： 1032.00

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

OseltamiviracidisanactivemetaboliteofOseltamivir,whichisapotentandselectiveinhibitorofinfluenzaAandBvirusneuraminidases.

CustomerValidation

•ACSNano.2014Jun24;8(6):5468-77.
•Oncotarget.2017Sep15;8(47):83142-83154.
•EurJMedChem.2017Dec1;141:648-656.
•AntimicrobAgentsChemother.2015Aug;59(8):4962-73.
•AntiviralRes.2017Jul;143:106-112.
•AntiviralRes.2016May;129:81-92.

•AntiviralRes.2016Mar;127:68-78.
•AntiviralRes.2014Nov;111:69-77.
•JEnvironManage.2015Oct1;162:326-33.
•EurJPharmSci.2017Sep28;111:167-176.
•EurJPharmSci.2015Jul8;78:47-53.
•Molecules.2017Nov18;22(11).pii:E1998.
•Molecules.2016Aug26;21(9).pii:E1133.
•PLoSOne.2016May27;11(5):e0156400.
•PLoSOne.2014Oct21;9(10):e110631.
•BiomedPharmacother.2017Oct27;97:385-394.
•BiomedPharmacother.2017Jul5;93:636-645.
•FEBSOpenBio.2013Oct29;3:484-9.
•ArchVirol.2014Dec;159(12):3269-78.
•EvidBasedComplementAlternatMed.2015;2015:917670.

Description

OseltamiviracidisanactivemetaboliteofOseltamivir,whichisapotentandselectiveinhibitorofinfluenzaAandBvirusneuraminidases.

IC₅₀&Target

InfluenzaAandB^[1]

InVitro

Oseltamiviracidinhibitsvirusreplicationinvitroandinvivo.InfluenzaBandA/H1N1virusesappearetobesensitivetoOseltamivir(meanBIC₅₀value:13nM;meanH1N1IC₅₀value:1.34nM),whileA/H1N2andA/H3N2virusesaremoresensitivetoOseltamivir(meanH3N2IC₅₀value:0.67nM;meanH1N2IC₅₀value:0.9nM)^[1].InneuraminidasesinhibitionassayswithinfluenzaAviruses,themedian50%inhibitoryconcentration(IC₅₀)ofRWJ-270201(approximately0.34nM)iscomparabletothatofOseltamivircarboxylate(0.45nM)ForinfluenzaBvirusisolates,theIC₅₀ofRWJ-270201(1.36nM)iscomparabletothatofZanamivir(2.7nM)andlessthanthatofOseltamivircarboxylate(8.5nM)^[2].

InVivo

Oseltamivir(0.1,1,or10mg/kg/day,twicedailybyoralgavage)producesadose-dependentantiviraleffectagainstVietnam/1203/04(VN1203/04)virus.The5-dayregimenat10mg/kg/dayprotects50%ofmice;deathsinthistreatmentgrouparedelayedandindicatedthereplicationofresidualvirusafterthecompletionoftreatment.Eight-dayregimensimprovedOseltamivirefficacy,anddosagesof1and10mg/kg/daysignificantlyreducedvirustitersinorgansandprovided60%and80%survivalrates,respectively^[3].Inthepharmacokineticstudy,aftertheoraladmiNISTrationof1,000mg/kgOseltamivir,peakplasmaconcentrationsarereachedat2hpostdoseforOseltamivirand8hforOseltamivircarboxylate(OC).RatsareexposedtoOseltamiviroverthewholesamplingintervalandhada~2.7-fold-higherrateofexposuretoOCthanOseltamivir.InCSF,peakconcentrationsarereachedat2hpostdoseforOseltamivirand6hforOC.CSF/plasmaexposureratios(AUC_0-8h)are~0.07forOseltamivirand0.007forOC.Inperfusedbrainsamples,peakconcentrationsarereachedat8hpostdoseforOseltamivirand6hforOC.Brain/plasmaexposureratios(AUC_0-8h)of~0.12forOseltamivirand0.01forOCarerecorded.CorrespondingCSF/brainexposureratiosrangedbetween~0.55and0.64forbothanalytes.AfurthergroupofanimalsthatreceivedasingleoraladministrationofOseltamiviratalowerdoseproducedsimilarresults^[4].

ClinicalTrial

ViewMoreCollapse

References

[1].FerrarisO,etal.Sensitivityofinfluenzavirusestozanamivirandoseltamivir:astudyperformedonvirusescirculatinginFrancepriortotheintroductionofneuraminidaseinhibitorsinclinicalpractice.AntiviralRes.2005Oct;68(1):43-8.
[2].GubarevaLV,etal.Comparisonoftheactivitiesofzanamivir,oseltamivir,andRWJ-270201againstclinicalisolatesofinfluenzavirusandneuraminidaseinhibitor-resistantvariants.AntimicrobAgentsChemother.2001Dec;45(12):3403-8.
[3].YenHL,etal.VirulencemaydeterminethenecessarydurationanddosageofoseltamivirtreatmentforhighlypathogenicA/Vietnam/1203/04influenzavirusinmice.JInfectDis.2005Aug15;192(4):665-72.
[4].HoffmannG,etal.Nonclinicalpharmacokineticsofoseltamivirandoseltamivircarboxylateinthecentralnervoussystem.AntimicrobAgentsChemother.2009Nov;53(11):4753-61.

AnimalAdministration ^[3]^[4]	OseltamivirisdissolvedinsterilePBS(Mice)^[3]. Mice^[3] Female6-week-oldBALB/cmiceareanesthetizedwithisofluoraneandintranasallyinoculatedwith50μLof10-foldserialdilutionsofVN1203/04virusinPBS.Themouselethaldose(MLD₅₀)iscalculatedaftera16-dayobservationperiod.Oseltamivirisadministeredbyoralgavagetwicedailyfor5or8daystogroupsof10miceatdosagesof0.1,1,and10mg/kg/day.Control(infectedbutuntreated)micereceivedsterilePBS(placebo)onthesameschedule.FourhoursafterthefirstdoseofOseltamivir,themiceareinoculatedintranasallywith5MLD₅₀ofVN1203/04virusin50μLofPBS.Survivalandweightchangeareobservedfor24days.Virustitersinthemouseorgansaredeterminedondays3,6,and9afterinoculation.Threemicefromeachexperimentalandplacebogrouparekilled,andthelungsandbrainsareremoved.TheorgansarehomogenizedandsUSPendedin1mLofPBS.Thecellulardebrisisclearedbycentrifugationat2000gfor5min.Thelimitofvirusdetectionis0.75log₁₀EID₅₀.Forcalculationofthemean,sampleswithavirustiter<0.75>₁₀EID₅₀/mLareassignedavalueof0.VirustitersineachorganarecalculatedbyuseofthemethodofReedandMuenchandareexpressedasmeanlog₁₀EID₅₀/mL±SE. Rat^[4] SeveralstudiesareperformedtocharacterizethepharmacokineticsofOseltamivirandOCintheplasma,cerebrospinalfluid(CSF),andbrainofSprague-Dawleyratsfollowingsingle-dosebolusadministrationofOseltamivir(intravenous[i.v.]andoral)andOC(i.v.).Inthei.v.studies,nonfastedadultrats(twogroupsof35animalsforeachtestsubstance)receivedadoseof30mg/kgbodyweightofeitherOseltamivirorOseltamivircarboxylate(OC)inaqueoussolutionwithsodiumchloride(0.9%;pH4.0)viaslowinjectionintothetailveinover20to30s.Inbothi.v.studies,pharmacokineticsamplingtookplaceat5minandat0.25,0.5,1,2,4,and8hpostdose(fourorfiverats/timepoint).MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.
References	[1].FerrarisO,etal.Sensitivityofinfluenzavirusestozanamivirandoseltamivir:astudyperformedonvirusescirculatinginFrancepriortotheintroductionofneuraminidaseinhibitorsinclinicalpractice.AntiviralRes.2005Oct;68(1):43-8. [2].GubarevaLV,etal.Comparisonoftheactivitiesofzanamivir,oseltamivir,andRWJ-270201againstclinicalisolatesofinfluenzavirusandneuraminidaseinhibitor-resistantvariants.AntimicrobAgentsChemother.2001Dec;45(12):3403-8. [3].YenHL,etal.VirulencemaydeterminethenecessarydurationanddosageofoseltamivirtreatmentforhighlypathogenicA/Vietnam/1203/04influenzavirusinmice.JInfectDis.2005Aug15;192(4):665-72. [4].HoffmannG,etal.Nonclinicalpharmacokineticsofoseltamivirandoseltamivircarboxylateinthecentralnervoussystem.AntimicrobAgentsChemother.2009Nov;53(11):4753-61.

AnimalAdministration
^[3]^[4]

OseltamivirisdissolvedinsterilePBS(Mice)^[3].

Mice^[3]
Female6-week-oldBALB/cmiceareanesthetizedwithisofluoraneandintranasallyinoculatedwith50μLof10-foldserialdilutionsofVN1203/04virusinPBS.Themouselethaldose(MLD₅₀)iscalculatedaftera16-dayobservationperiod.Oseltamivirisadministeredbyoralgavagetwicedailyfor5or8daystogroupsof10miceatdosagesof0.1,1,and10mg/kg/day.Control(infectedbutuntreated)micereceivedsterilePBS(placebo)onthesameschedule.FourhoursafterthefirstdoseofOseltamivir,themiceareinoculatedintranasallywith5MLD₅₀ofVN1203/04virusin50μLofPBS.Survivalandweightchangeareobservedfor24days.Virustitersinthemouseorgansaredeterminedondays3,6,and9afterinoculation.Threemicefromeachexperimentalandplacebogrouparekilled,andthelungsandbrainsareremoved.TheorgansarehomogenizedandsUSPendedin1mLofPBS.Thecellulardebrisisclearedbycentrifugationat2000gfor5min.Thelimitofvirusdetectionis0.75log₁₀EID₅₀.Forcalculationofthemean,sampleswithavirustiter<0.75>₁₀EID₅₀/mLareassignedavalueof0.VirustitersineachorganarecalculatedbyuseofthemethodofReedandMuenchandareexpressedasmeanlog₁₀EID₅₀/mL±SE.
Rat^[4]
SeveralstudiesareperformedtocharacterizethepharmacokineticsofOseltamivirandOCintheplasma,cerebrospinalfluid(CSF),andbrainofSprague-Dawleyratsfollowingsingle-dosebolusadministrationofOseltamivir(intravenous[i.v.]andoral)andOC(i.v.).Inthei.v.studies,nonfastedadultrats(twogroupsof35animalsforeachtestsubstance)receivedadoseof30mg/kgbodyweightofeitherOseltamivirorOseltamivircarboxylate(OC)inaqueoussolutionwithsodiumchloride(0.9%;pH4.0)viaslowinjectionintothetailveinover20to30s.Inbothi.v.studies,pharmacokineticsamplingtookplaceat5minandat0.25,0.5,1,2,4,and8hpostdose(fourorfiverats/timepoint).MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

[1].FerrarisO,etal.Sensitivityofinfluenzavirusestozanamivirandoseltamivir:astudyperformedonvirusescirculatinginFrancepriortotheintroductionofneuraminidaseinhibitorsinclinicalpractice.AntiviralRes.2005Oct;68(1):43-8.
[2].GubarevaLV,etal.Comparisonoftheactivitiesofzanamivir,oseltamivir,andRWJ-270201againstclinicalisolatesofinfluenzavirusandneuraminidaseinhibitor-resistantvariants.AntimicrobAgentsChemother.2001Dec;45(12):3403-8.
[3].YenHL,etal.VirulencemaydeterminethenecessarydurationanddosageofoseltamivirtreatmentforhighlypathogenicA/Vietnam/1203/04influenzavirusinmice.JInfectDis.2005Aug15;192(4):665-72.
[4].HoffmannG,etal.Nonclinicalpharmacokineticsofoseltamivirandoseltamivircarboxylateinthecentralnervoussystem.AntimicrobAgentsChemother.2009Nov;53(11):4753-61.

MolecularWeight

284.35

Formula

C₁₄H₂₄N₂O₄

CASNo.

187227-45-8

Storage

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

Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

H₂O:≥56mg/mL

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

Purity:98.60%

SelectBatch: