P163-0892-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEP163-0892Cat.No.:HY-150972CASNo.:1574576-45-6分⼦式:C₁₉H₂₀N₂O₃S分⼦量:356.44作⽤靶点:Fungal作⽤通路:Anti-infection储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性P163-0892⼀种对Cryptococcus种具有强选择性的抗真剂（antifungal）。P163-0892被预测具有中等程度的⾎脑屏障透过性。体外研究P163-0892(0-32μg/mL;48h)showsantifungalactivitywithaMICof0.25μg/mLand0.5μg/mLagainstCryptococcusneoformansandCryptococcusgattii,respectively[1].P163-0892hasgoodaqueoussolubility[1].P163-0892hasnocytotoxicityandnoobviouscardiotoxicity[1].体内研究P163-0892(10mg/kg;5days)significantlyextendsthesurvivaloflarvaeinfectedwitheitherC.neoformansorC.gattii[1].AnimalModel:WaxmothlarvainfectedwithC.neoformansH99orC.gattiiWM178[1]Dosage:10mg/kgAdministration:5daysResult:Increasedthesurvivalrateoflarvae.AnimalModel:MaleSprague–Dawleyratsweighing200–250g[1]Dosage:2mg/kgor5mg/kgAdministration:Intravenousororaladministration(PharmacokineticAnalysis)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:PharmacokineticParametersofP163-0892a[1]routedose(mg/kg)T1/2(h)Tmax(h)AUC0-inf(h•ng/mL)Cl(mL/h/kg)MRT0-t(h)Vdss(L/kg)BA(%)iv2mg/kg7.617491722.637.12po5mg/kg15.33.17NR3.83NR0.8aAbbreviations:iv,intravenous;po,peros;T1/2,half-lifeeliminationinhours;Tmax,timeofmaximalconcentrationinhours;AUC,areaunderthecurve;Cl,clearance;MRT,meanresidencetime;Vdss,volumeofdistributionatthesteadystate;BA,bioavailability;NR,notreportable;n=3.REFERENCES[1].LiL,etal.DiscoveryofNovel7-Hydroxy-5-oxo-4,5-dihydrothieno[3,2-b]pyridine-6-carboxamideDerivativeswithPotentandSelectiveAntifungalActivityagainstCryptococcusSpecies.JMedChem.2022Aug3.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-82