1R-3S-THCCA-Asn-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE(1R,3S)-THCCA-AsnCat.No.:HY-151146分⼦式:C₂₄H₂₄N₄O₆分⼦量:464.47作⽤靶点:Thrombin作⽤通路:MetabolicEnzyme/Protease储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性(1R,3S)-THCCA-Asn(4j)⼀种选择性凝⾎酶(thrombin)抑制剂，其IC50值在0.07~0.14μM的范内。(1R,3S)-THCCA-Asn具有抗⾎栓形成活性。体外研究(1R,3S)-THCCA-Asn(4j)(0.001-500μM)hasanti-plateletaggregationactivitywiththeIC50valuerangedfrom0.07μMto0.14μM,andinhibitsADP-inducedplateletaggregationbylessthan20%aswellasAA-inducedplateletaggregationbylessthan10%[1].(1R,3S)-THCCA-Asn(4j)(0.001-1000μM,48h)haslesstoxictomammaliancellssuchaslivercell,colonmucosacellandhumandermalfibroblastsinvitro[1].CellProliferationAssay[1]CellLine:Livercell(L02),colonmucosacell(NCM460)andhumandermalfibroblastscell(NHDF)Concentration:0.001-1000μMIncubationTime:48hoursResult:ShowedthattheIC50valuesforcellviabilitywereallhigherthan125μM.体内研究(1R,3S)-THCCA-Asn(4j)(p.o.,0.001-1nM/kg)canactagainstthrombosisofratsinadose-dependentmannerwithnotoxicsideeffects[1].AnimalModel:MaleSD(SpragueDawley)ratsweighing250-300g[1]Dosage:0.001,0.01,1nM/kg1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAdministration:p.o.Result:Resultedinareductioninthrombusweightof19.19mgatthedoseof1nM/kgcomparedtotheuntreatedthrombusweightofabout30mg.REFERENCES[1].XiaoyiZhang,etal.(1R,3S)-THCCA-Asn:Toshowthediscoveryofselectiveinhibitorofthrombinbysuccessfullycombiningvirtualscreeningandbiologicalassay,EuropeanJournalofMedicinalChemistry,Volume242,2022,114681.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792