Icotro kinra-acetate-JNJ-77242113-acetate-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEIcotrokinraacetateCat.No.:HY-P10587ASynonyms:JNJ-77242113acetate;JNJ-2113acetate;PN-235acetate分⼦式:C₉₀H₁₂₀N₂₀O₂₂S₂·xC₂H₄O₂Sequence:Ac-Pen-Asn-Thr-Trp(7-Me)-Lys(Ac)-Pen-Phe(4-aminoethoxy)-2Nal-ThpGly-Glu-Asn-3Pal-Sar-NH2(Pen1&Pen6bridge)作⽤靶点:InterleukinRelated;STAT;IFNAR作⽤通路:Immunology/Inflammation;JAK/STATSignaling;StemCell/Wnt储存⽅式:Sealedstorage,awayfrommoisturePowder-80°C2years-20°C1yearInsolvent-80°C6months-20°C1monthBIOLOGICALACTIVITY⽣物活性Icotrokinra(JNJ-77242113)acetate⼀种⼝服有效的IL-23受体(IL-23receptor)选择性拮抗剂。Icotrokinra可抑制外周⾎单核细胞(PMBC)中IL-23诱导的STAT3磷酸化(IC50=5.6pM)，并抑制NK细胞中IL-23诱导的⼲扰素IFN-γ的产⽣，IC50为18.4pM。Icotrokinraacetate在TNBS诱导的⼤⿏结肠炎模型中表现出抗炎活性。Icotrokinraacetate可⽤于银屑病、银屑病关节炎和炎症性肠病的研究[1]。IC50&TargetIL-237.1pM(Kd)体内研究Icotrokinra(0.03-10mg/kg;p.o.;oncedailyfor7days)acetatereducesthecolonweight-to-lengthratioandalleviatesweightlossinratswithTNBS-inducedcolitis[1].Icotrokinra(1-30mg/kg;p.o.;twicedailyfor3days)acetatepreventsIL-23-inducedupregulationofIL-17AandIL-22inaratskininflammationmodelatdosesgreaterthan10mg/kg[1].REFERENCES[1].FourieAM,etal.,JNJ-77242113,ahighlypotent,selectivepeptidetargetingtheIL-23receptor,providesrobustIL-23pathwayinhibitionuponoraldosinginratsandhumans.SciRep.2024Jul30;14(1):17515.McePdfHeight1/1MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792/p>