Etrolizumab-rhuMAb-Beta7-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEtrolizumabCat.No.:HY-P9984CASNo.:1044758-60-2Synonyms:rhuMAbBeta7;RG7413;PRO145223作⽤靶点:Integrin作⽤通路:Cytoskeleton储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Etrolizumab(rhuMAbBeta7)⼀种肠道选择性抗-β7整合素单克隆抗体。Etrolizumab针对α4β7和αEβ7整合素的β7亚的特异性靶向药物。Etrolizumab可⽤于炎症性肠病(IBD)的研究。IC50&Targetα4β7αEβ7体外研究Etrolizumab(rhuMAbBeta7)bindstheβ7subunitofbothα4β7andαEβ7integrinswithhighaffinity,withKdvaluesof18nM,1800pM,181pM,116pM,57pM,31.7pM,and25.7pMforHumanα4β7,HumanαEβ7-293,Mouseα4β7-38C13,Humanα4β7-293,RabbitPBLs,HumanPBLs,andCynoPBLs,respectively[1].Etrolizumab(RPMI8866cellsandαEβ7-293cells)blockstheinteractionofα4β7withitscognateligandsMAdCAM-1andVCAM-1withIC50valuesof0.075and0.089nM,respectively,andblockstheinteractionbetweenαEβ7anditsligandE-cadherinwithanIC50valueof3.96nM[1].体内研究Etrolizumab(rhuMAbBeta7;5mg/kg;i.v.;once;normalfemaleBALB/cmice)decreasesβ7integrinsonTlymphocytes[2].Etrolizumab(200µg(100µL);i.p.;once)inhibitslymphocytehomingintheCD45RBhighTcell-reconstitutedSCIDmousemodelofcolitis[2].AnimalModel:NormalfemaleBALB/cmice(17-21g)[2]Dosage:5mg/kgAdministration:Intravenousinjection;onceResult:Had98.3%ofintraepithelialCD8+T-cellβ7integrinreceptorsand90.0%of1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEintraepithelialCD4+T-cellβ7integrinreceptorsafter24h.AnimalModel:SCIDmousemodelofcolitis[2]Dosage:200µg(100µL)Administration:Intraperitonealinjection;onceResult:Blockedlymphocyterecruitmentandhomingtotheinflamedcolon.REFERENCES[1].TangMT,et,al.Reviewarticle:nonclinicalandclinicalpharmacology,pharmacokineticsandpharmacodynamicsofetrolizumab,ananti-β7integrintherapyforinflammatoryboweldisease.AlimentPharmacolTher.2018Jun;47(11):1440-1452.[2].StefanichEG,et,al.Ahumanizedmonoclonalantibodytargetingtheβ7integrinselectivelyblocksintestinalhomingofTlymphocytes.BrJPharmacol.2011Apr;162(8):1855-70.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuse