Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELRRK2-IN-5Cat.No.:HY-151441分?式:C??H??F?N?O?S分?量:472.55作?靶點:LRRK2作?通路:Autophagy儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性LRRK2-IN-5(compound25)?種?服有效的選擇性富含亮氨酸重復蛋?激酶2因(LRRK2)抑制劑，抑制GSLRRK2和WTLRRK2的IC50值分別為1.2和16μM。LRRK2-IN-5抑制LRRK2Ser1292和Ser925的?磷酸化。LRRK2-IN-5可以通過?腦屏障。IC50&TargetIC50:1.2(GSLRRK2)and16μM(GSLRRK2)[1]體外研究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.體內研究LRRK2-IN-5(compound25;0.5mg/kg(i.v.)and5mg/kg(p.o.);CD-1mice)hasgoodpharmacokineticparametershighandhighbioavailability[1].AnimalModel:CD-1mice[1]1/2MasterofBioactiveMolecules—您?邊的抑制劑?師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].Le?niakRK,et,al.Discoveryofazaspirocyclic1H-3,4,5-TrisubstituedpyrazolesasnovelG2019S-LRRK2selectivekinaseinhibitors.EurJMedChem.2022Nov15;242:114693.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021-589559