JNJ-47965567-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEJNJ-47965567Cat.No.:HY-101418CASNo.:1428327-31-4分⼦式:C₂₈H₃₂N₄O₂S分⼦量:488.64作⽤靶点:P2XReceptor作⽤通路:MembraneTransporter/IonChannel储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:25mg/mL(51.16mM;ultrasonicandwarmingandheatto50°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0465mL10.2325mL20.4650mL5mM0.4093mL2.0465mL4.0930mL10mM0.2046mL1.0232mL2.0465mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存⽅式和期限。BIOLOGICALACTIVITY⽣物活性JNJ-47965567⼀种中枢通透性、⾼亲和⼒、选择性的P2X7拮抗剂，对⼈和⼤⿏P2X7作⽤的pKi值分别为7.9和8.7。JNJ-47965567可⽤于探讨中枢P2X7在中枢神经系统病理⽣理模型中的作⽤[1]。IC50&TargetpKi:7.9(huamanP2X7),8.7(ratP2X7)[1]体外研究JNJ-47965567exhibitshighaffinityforhumanandratP2X7inmembranepreparationsof1321N1cells[1].JNJ-47965567doesnotblockIL-6andTNF-αrelease,underidenticalconditions(LPSandBZ-ATP)usedfor1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEIL-1βandIL-18release[1].JNJ-47965567attenuatesIL-1βreleasewithpIC50sof6.7±0.07(humanblood),7.5±0.07(humanmonocytes)and7.1±0.1(ratmicroglia),respectively,innativesystems[1].体内研究JNJ-47965567(30-100mg/kg;s.c.)attenuatesIL-1βreleaseinducedbyBz-ATP[1].JNJ-47965567(30ꢀmg/kg)attenuatesamphetamine-inducedhyperactivityandexhibitsmodest,yetsignificantefficacyintheratmodelofneuropathicpain[1].AnimalModel:MaleSpragueDawleyrats[1]Dosage:30mg/kg,100mg/kgAdministration:Subcutaneousinjection;30minutespriortoBz-ATPinfusionResult:SignificantlyattenuatedIL-1βreleaseat100mg/kg,withnoeffectat30mg/kgdosegroup.REFERENCES[1].BhattacharyaA,etal.PharmacologicalcharacterizationofanovelcentrallypermeableP2X7receptorantagonist:JNJ-47965567.BrJPharmacol.2013Oct;170(3):624-40.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:40