Compstatin-TFA-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECompstatinTFACat.No.:HY-P1036A分⼦式:C₆₈H₁₀₀F₃N₂₃O₁₉S₂分⼦量:1664.79SequenceShortening:ICVVQDWGHHRCT-NH2(Disulfidebridge:Cys2-Cys12)作⽤靶点:ComplementSystem作⽤通路:Immunology/Inflammation储存⽅式:Protectfromlight,storedundernitrogenPowder-80°C2years-20°C1yearInsolvent-80°C6months-20°C1monthBIOLOGICALACTIVITY⽣物活性CompstatinTFA⼀个13残环肽，补体系统C3的有效抑制剂，具有物种特异性。CompstatinTFA结合到狒狒的C3，并对狒狒⾎液中的蛋⽩⽔解裂解具有抗性（类似⼈类）。CompstatinTFA只抑制灵长类补体系统的激活。CompstatinTFA对补体经典途径和旁路途径的IC50值分别为63μM和12μM。体外研究Compstatinexhibitsaninvitrohalf-lifeinhumanbloodofabout2hr[2].Insolution,compstatinformsaβ-turnatresiduesGln-5–Gly-8withthedisulfidebridgeCys-2–Cys12,residuesIle-1–Val-4,andThr-13,formingahydrophobiccluster[3].体内研究Compstatin(21mg/kg)producescompleteinhibitionwhengivenasacombinationofbolusinjectionandinfusion.Compstatincompletelyinhibitsinvivoheparin/protamine-inducedcomplementactivationwithoutadverseeffectsonheartrateorsystemicarterial,centralvenous,andpulmonaryarterialpressures[1].Compstatinisstableinbaboonplasmaformorethan24h[1].PigxenograftssurvivalissignificantlylongerintheCompstatinperfusedgroupthaninthecontrolgroup[2].AnimalModel:Juvenilebaboons(P.Anubis)weighing10.5-28.8kg[1].Dosage:50,25mg/kg60minafterheparinand2minbeforeprotamine.Administration:Abolusinjection.1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:Completelyinhibitedcomplementactivationinducedbyheparin–protaminecomplexes.户使⽤本产品发表的科研⽂献•JMaterChemB.2019,7,4207-4216.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SoulikaAM,etal.Inhibitionofheparin/protaminecomplex-inducedcomplementactivationbyCompstatininbaboons.ClinImmunol.2000Sep;96(3):212-21.[2].FianeAE,etal.Compstatin,apeptideinhibitorofC3,prolongssurvivalofexvivoperfusedpigxenografts.Xenotransplantation.1999Feb;6(1):52-65.[3].BertJCJanssen,etal.StructureofcompstatinincomplexwithcomplementcomponentC3crevealsanewmechanismofcomplementinhibition.JBiolChem.2007Oct5;282(40):29241-7.[4].ASahu,etal.InhibitionofhumancomplementbyaC3-bindingpeptideisolatedfromaphage-displayedrandompeptidelibrary.JImmunol.1996Jul15;157(2):884-91.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forre