Ganciclovir-hydrate-BW-759-hydrate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGanciclovirhydrateCat.No.:HY-13637BCASNo.:1359968-33-4Synonyms:BW-759hydrate;2'-Nor-2'-deoxyguanosinehydrate分⼦式:C₉H₁₅N₅O₅分⼦量:273.25作⽤靶点:CMV;HSV;Antibiotic;NucleosideAntimetabolite/Analog作⽤通路:Anti-infection;CellCycle/DNADamage储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Ganciclovir(BW759)hydrate⼀种核苷类似物和⼝服抗病毒药物，对CMV具有抗病毒活性。Ganciclovirhydrate在体外对疹病毒(herpesgroup)和其他⼀些DNA病毒也具有抗病毒活性。Ganciclovirhydrate抑制⼈类疹病毒(HSV1型和2型，CMV)和腺病毒⾎型1、2、4、6、8、10、19、22和28的体外复制。Ganciclovirhydrate对猫1型疹病毒(FHV-1)的IC50为5.2μM，可透过⼤脑屏障。IC50&TargetCMVHSV-1HSV-2FHV-15.2μM(IC50)体外研究Ganciclovir(BW759)isanacyclicdeoxyguanosineanalogstructurallysimilartoacyclovirbutwithsuperioractivityagainstCMV.ThemedianGanciclovirconcentrationrequiredtoinhibitviralreplicationby50percentis2.15μMversus72μMforacyclovir[4].TheprimarymechanismofGancicloviractionagainstCMVisinhibitionofthereplicationofviralDNAbyganciclovir-5'-triphosphate(ganciclovir-TP).ThisinhibitionincludesaselectiveandpotentinhibitionoftheviralDNApolymerase.Ganciclovirismetabolizedtothetriphosphateformbyprimarilythreecellularenzymes:adeoxyguanosinekinaseinducedbyCMV-infectedcells;guanylatekinase;andphosphoglyceratekinase[5].体内研究Ganciclovir(BW759)(50mg/kg;i.p.;twiceadayforfiveinjections)significantlydecreaseswhitebloodcells,redbloodcellsandplateletsinnewbornmice,andcandiffuseintothebrainandtheperilymphaticspaceoftheinnerear[3].Ganciclovir(1-80mg/kg;i.h.;dailyfor5days)delaysmurinecytomegalovirus(MCMV)-inducedwastingsyndromeandmortality[6].1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:Non-inbredOncinsFrance1(OF1)miceandalbinoratsnon-immunizedforMCMV[3]Dosage:50mg/kgAdministration:Intraperitonealinjection,twiceadayforfiveinjections(mice)or3days(adultrats)(PharmacokineticStudy)Result:Inadultrats,theintracochleardiffusionofGanciclovirwasshowntoachievethesameconcentrationasinblood.Ingestatingmice,transplacentaldiffusionwasobserved,withafetal-to-maternalbloodratioof0.5.Innewbornmice,theplasmaconcentrationprofileofGanciclovirshowedapeakat2hfollowedbyagradualdecrease.Inadultmice,theconcentrationpeakedat1h,butbecameundetectableby2hafterinjection.Significantlydecreasedwhitebloodcells,redbloodcellsandplateletsinnewbornmice.AnimalModel:FemaleSCIDmiceinoculatedwithMCMV[6]Dosage:0,1,10,80and160mg/kgAdministration:Subcutaneousinjection,oncedailyfor5daysResult:Dosedependentlydelayedthewastingsyndromeandmortalityinadoserangeupto80mg/kgperday,whereasadoseof160mg/kgperdayinducedreversibleside-effects.户使⽤本产品发表的科研⽂献•Cell.2020Nov25;183(5):1402-1419.e18.•BrainBehavImmun.2019Aug;80:394-405.•JNanobiotechnology.2022Jul20;20(1):340.•Cells.2019Dec20;9(1):31.•JVirol.2017Jan18;91(3).pii:e02152-16.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].FauldsD,etal.Ganciclovir.Areviewofitsantiviralactivity,pharmacokineticpropertiesandtherapeuticefficacyincytomegalovirusinfections.Drugs.1990;39(4):597-638.[2].MaggsDJ,etal.Invitroefficacyofganciclovir,cidofovir,penciclovir,foscarnet,idoxuridine,andacycloviragainstfelineherpesvirustype-1.AmJVetRes.2004Apr;65(4):399-403.[3].BoujemlaI,etal.Pharmacokineticsandtissuediffusionofganciclovirinmiceandrats.AntiviralRes.2016;132:111-115.[4].FletcherCV,etal.Evaluationofganciclovirforcytomegalovirusdisease.DICP.1989Jan;23(1):5-12.[5].MatthewsT,etal.Antiviralactivityandmechanismofactionofganciclovir.RevInfectDis.1988Jul-Aug;10Suppl3:S490-4.[6].DuanJ,ParisW,KiblerP,BousquetC,LiuzziM,CordingleyMG.Doseandduration-dependenceofganciclovirtreatmentagainst2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEmurinecytomegalovirusinfectioninseverecombinedimmunodeficientmice.AntiviralRes.1998;39(3):189-1