NDT-9513727-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrariesNDT9513727Cat.No.:HY-110060CASNo.:439571-48-9分⼦式:C₃₆H₃₅N₃O₄分⼦量:573.68作⽤靶点:ComplementSystem作⽤通路:Immunology/Inflammation储存⽅式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验Ethanol:57mg/mL(99.36mM;Needultrasonicandwarming)DMSO:57mg/mL(99.36mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7431mL8.7157mL17.4313mL5mM0.3486mL1.7431mL3.4863mL10mM0.1743mL0.8716mL1.7431mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存⽅式和期限。BIOLOGICALACTIVITY⽣物活性NDT9513727⼀种⾼效的，选择性的，具有⼝服活性的，竞争性的⼈C5aR反向激动剂，其IC50值为11.6nM。NDT9513727可⽤于⼈炎症疾病的研究[1]。IC50&TargetIC50:11.6nM(humanC5aR)[1]体外研究NDT9513727inhibitsC5a-stimulatedresponses,includingguanosine5'-3-O-(thio)triphosphatebinding,Ca2+mobilization,oxidativeburst,degranulation,cellsurfaceCD11bexpressionandchemotaxisinvariouscell1/3typeswithIC50sfrom1.1to9.2nM,respectively[1].体内研究NDT9513727(3-30mg/kg;p.o.)exhibitsadose-dependentinhibitionofhC5a-inducedneutropenia[1].NDT9513727exhibitsmoderateoralbioavailability(rat73%,monkey26%)andCmax(rat5.98μM,monkey830nM)followingoraladministration(rat50,monkey25.2mg/kg)[1].NDT9513727exhibitsmoderateplasmaeliminationhalf-lives(rat4.8,monkey7.9h)duetolowplasmaclearance(1.4L/h/kgand3.8l/h/kgrespectively)followingoraladministration(rat50,monkey25.2mg/kg)[1].AnimalModel:Six-week-oldMongoliangerbils[1]Dosage:1mg/kg,3mg/kg,10mg/kg,30mg/kgAdministration:OraladministrationResult:SignificantlyinhibitedhC5a-inducedneutropeniaat3mg/kg,10mg/kg,30mg/kg.AnimalModel:Rat[1]Dosage:50mg/kgAdministration:OraladministrationResult:Oralbioavailability(73%),Cmax(5.98μM),T1/2(4.8h).AnimalModel:Monkey[1]Dosage:25.2mg/kgAdministration:OraladministrationResult:Oralbioavailability(26%),Cmax(830nM),T1/2(7.9h).REFERENCES[1].RobbinMBrodbeck,etal.IdentificationandcharacterizationofNDT9513727[N,N-bis(1,3-benzodioxol-5-ylmethyl)-1-butyl-2,4-diphenyl-1H-imidazole-5-methanamine],anovel,orallybioavailableC5areceptorinverseagonist.JPharmacolExpTher.2008Dec;327(3):898-909.McePdfHeight2/3MedChemExpress(MCE)只为有资质的科研机构、医药企业