Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECompstatinTFACat.No.:HY-P1036A分?式:C??H???F?N??O??S?分?量:1664.79SequenceShortening:ICVVQDWGHHRCT-NH2(Disulfidebridge:Cys2-Cys12)作?靶點(diǎn):ComplementSystem作?通路:Immunology/Inflammation儲(chǔ)存?式:Protectfromlight,storedundernitrogenPowder-80°C2years-20°C1yearInsolvent-80°C6months-20°C1monthBIOLOGICALACTIVITY?物活性CompstatinTFA?個(gè)13殘環(huán)肽，補(bǔ)體系統(tǒng)C3的有效抑制劑，具有物種特異性。CompstatinTFA結(jié)合到狒狒的C3，并對(duì)狒狒?液中的蛋??解裂解具有抗性（類似?類）。CompstatinTFA只抑制靈長(zhǎng)類補(bǔ)體系統(tǒng)的激活。CompstatinTFA對(duì)補(bǔ)體經(jīng)典途徑和旁路途徑的IC50值分別為63μM和12μM。體外研究Compstatinexhibitsaninvitrohalf-lifeinhumanbloodofabout2hr[2].Insolution,compstatinformsaβ-turnatresiduesGln-5–Gly-8withthedisulfidebridgeCys-2–Cys12,residuesIle-1–Val-4,andThr-13,formingahydrophobiccluster[3].體內(nèi)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?邊的抑制劑?師www.MedChemEResult:Completelyinhibitedcomplementactivationinducedbyheparin–protaminecomplexes.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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