Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEP163-0892Cat.No.:HY-150972CASNo.:1574576-45-6分?式:C??H??N?O?S分?量:356.44作?靶點:Fungal作?通路:Anti-infection儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性P163-0892?種對Cryptococcus種具有強(qiáng)選擇性的抗真劑（antifungal）。P163-0892被預(yù)測具有中等程度的?腦屏障透過性。體外研究P163-0892(0-32μg/mL;48h)showsantifungalactivitywithaMICof0.25μg/mLand0.5μg/mLagainstCryptococcusneoformansandCryptococcusgattii,respectively[1].P163-0892hasgoodaqueoussolubility[1].P163-0892hasnocytotoxicityandnoobviouscardiotoxicity[1].體內(nèi)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?邊的抑制劑?師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