Inclacumab-Anti-Human-selectin-P-Recombinant-Antibody-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEInclacumabCat.No.:HY-P99263CASNo.:1256258-86-2Synonyms:Anti-HumanselectinPRecombinantAntibody作⽤靶点:Others作⽤通路:Others储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Inclacumab(Anti-HumanselectinPRecombinantAntibody)⼈化的IgG4单克隆抗体选择性的靶向P-selectin，Kd值为9.9nM。Inclacumab抑制P-selectin糖蛋⽩配体1(PSGL-1)模拟肽与P-selectin结合，IC50值为1.9µg/mL。Inclacumab强烈的抑制细胞黏附。体外研究Inclacumab(0.4-40μg/mL;5min)significantlyreducesflowadhesionofP-SelectinwithWholeBlood(WB)andisolatedWhiteBloodCell(I-WBC)andshowsamorestrongereffectonisolatedwhitecells[1].InclacumabshowsgreatbindingaffinitytoP-selectinwithaKdvalueof9.9nM[2].InclacumabinhibitsPSGL-1mimeticpeptidebindingwithP-selectinwithanIC50valueof1.9µg/mL[2].InclacumabblockstheadhesionofPSGL-1expressingcellstoanimmobilizedP-selectinwithanIC50valueof430ng/mL[2].Inclacumab(0-100μg/mL;5min)dose-dependentlyinhibitsthrombinreceptor-activatingpeptide(TRAP)-inducedplatelet-leukocyteaggregates(PLA)levelswithanIC50valueof1.4μg/mL[3].体内研究Inclacumab(4mg/kg;s.c.once)reducesTRAP-andADP-inducedPLAlevelsincynomolgusmonkeys[3].Inclacumab(2-50mg/kg;i.v.;onceaweekfor13weeks)inhibitsTRAPinducedPLAlevelsincynomolgusmonkeys[3].AnimalModel:Cynomolgusmonkeys[3]Dosage:4mg/kgAdministration:Subcutaneousinjection;4mg/kg;onceResult:SignificantlyreducedTRAP-inducedPLAlevelsfrom25%to6%andsupressedPLAformation≥80%foratleast28daysposttreatment.Remainedplasmaconcentrations1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE>20μg/mLduringposttreatmentfor28days.SignificantlyinhibitedtheformationofADP(10μM)-inducedPLAs.AnimalModel:Cynomolgusmonkeys[3]Dosage:2,10,and50mg/kgAdministration:Intravenousinjection;oncedaily;for13weeksResult:InhibitedTRAP-inducedPLAandremainedconcentrationsatallthreedoselevelsarehigherthan20μg/mL.PersistedthefullinhibitionofPLAformationbetweendosingperiod.REFERENCES[1].TarasevM,etal.S107:P-SELECTININHIBITORINCLACUMABREDUCESCELLADHESIONINANIN-VITROASSAYSSHOWINGPOTENTIALFORPREVENTIONOFVASO-OCCLUSIONEVENTSINSICKLECELLDISEASE.Hemasphere.2022Jan31;6(Suppl):3-4.[2].XinGeng,etal.Inclacumab,aFullyHumanAnti-P-SelectinAntibody,DirectlyBindstoPSGL-1BindingRegionandDemonstratesRobustandDurableInhibitionofCellAdhesion.Blood(2020)136(Supplement1):10–11.[3].KlingD,etal.Pharmacologicalcontrolofplatelet-leukocyteinteractionsbythehumananti-P-selectinantibodyinclacumab--preclinicalandclinicalstudies.ThrombRes.2013May;131(5):401-10.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical