sALT629-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEsALT629Cat.No.:HY-179649CASNo.:484026-63-3分⼦式:C₁₃H₁₇N₅O₂分⼦量:275.31作⽤靶点:Bacterial作⽤通路:Anti-infection储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性sALT629⼀种有⼝服活性的抗结核剂，具有强效巨噬细胞内活性(EC50值为1.5μM)。sALT629在四种碳源中均表现出⼴谱抗结核分枝杆(Mycobacteriumtuberculosis，Mtb)活性，对耐药性结核分枝杆具有同等效⼒，且对缓慢复制和⾮复制的结核分枝杆均有活性。sALT629与恶唑烷酮类药物，如Linezolid(HY-10394)和Sutezolid(HY-10392)联合使⽤时，展现出协同活性。sALT629可⽤于结核病的研究。体外研究sALT629(0.96-12.5μM)exhibitsinhibitoryactivityagainstMtbculturedonfourcarbonsources(acetate,butyrate,cholesterol,glucose),withanEC50of1.5μMagainstintramacrophageMtb,anMICof0.8-1.7μMagainstmultidrug-resistant(MDR),extensivelydrug-resistant(XDR),andsingle-drug-resistantMtbstrains,andactivityagainstslow-replicatingandnonreplicatingMtb[1].sALT629(1.7-13.6μM;7days)showsdose-dependentbactericidalactivityagainstMtbin7H12cholesterolmedia[1].sALT629(20μM;7days)reducesCFUbyapproximately1.5-logintheHu-Coates100-daydormancymodelandby0.5-loginLoebel'snutritionallydeprivedmodel[1].sALT629(>40μM)showsnosignificantcytotoxicityagainstHEK293TandHepG2cells,withaSIgreaterthan23[1].sALT629exhibitssynergisticactivitywhencombinedwithoxazolidinonedrugs(Linezolid(HY-10394),Sutezolid(HY-10392))withanFICof0.5,additiveeffectswithdrugssuchasTBD11,TBA-7371(HY-19750),andQ203(HY-101040)(FIC=0.63-1.0),andnosignificantinteractionwithIsoniazid(HY-B0329)andotheragents(FIC>1.0)[1].体内研究sALT629(30-100mg/kgBID,or200mg/kgQD,p.o.,for4consecutivedays)exhibitsnosignificanttoxicityinCD-1mice,withnobodyweightlossorabnormalitiesinclinicalchemistryandhematologyindices[1].sALT629(100mg/kgBID,or200mg/kgQD,p.o.,for4consecutivedays)showsplasmaconcentrations1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEremainingaboveEC50forover24hours,andlungtissueexposureexceedsEC50[1].REFERENCES[1].YangB,etal.Design,Synthesis,andBiologicalEvaluationofTetrazol-2-yl-acetamidesasNovelAntitubercularAgents.ACSMedChemLett.2025Nov21;16(12):2444-2453.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch