LRRK2-IN-5-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELRRK2-IN-5Cat.No.:HY-151441分⼦式:C₂₄H₂₆F₂N₄O₂S分⼦量:472.55作⽤靶点:LRRK2作⽤通路:Autophagy储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性LRRK2-IN-5(compound25)⼀种⼝服有效的选择性富含亮氨酸重复蛋⽩激酶2因(LRRK2)抑制剂，抑制GSLRRK2和WTLRRK2的IC50值分别为1.2和16μM。LRRK2-IN-5抑制LRRK2Ser1292和Ser925的⾃磷酸化。LRRK2-IN-5可以通过⾎脑屏障。IC50&TargetIC50:1.2(GSLRRK2)and16μM(GSLRRK2)[1]体外研究LRRK2-IN-5(compound25;0-10000nM;24h;HEK293cells)hasexcellentpotencyandGS-LRRK2selectivity[1].CellViabilityAssay[1]CellLine:HEK293cellsConcentration:0,30,100,300,1000,3000,and10000nMIncubationTime:24hoursResult:ReducedGS-LRRK2pSer935andGS-LRRK2pSer1292autophosphorylationlevelsoverWT-LRRK2.体内研究LRRK2-IN-5(compound25;0.5mg/kg(i.v.)and5mg/kg(p.o.);CD-1mice)hasgoodpharmacokineticparametershighandhighbioavailability[1].AnimalModel:CD-1mice[1]1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEDosage:0.5mg/kg(i.v.)and5mg/kg(p.o.)Administration:IntravenousinjectionandoraladministrationResult:1.19RouteofAdministrationIVPODose(mg/kg)0.55AUCinf(μM*h)0.511.44Cmax(μM)0.610.60Tmax(h)0.080.50T1/2(h)0.451.46MRT(h)0.652.35CL(mL/min)34.3F(%)28REFERENCES[1].LeśniakRK,et,al.Discoveryofazaspirocyclic1H-3,4,5-TrisubstituedpyrazolesasnovelG2019S-LRRK2selectivekinaseinhibitors.EurJMedChem.2022Nov15;242:114693.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021-589559