NDT-9513727-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrariesNDT9513727Cat.No.:HY-110060CASNo.:439571-48-9分?式:C??H??N?O?分?量:573.68作?靶點:ComplementSystem作?通路:Immunology/Inflammation儲存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗Ethanol:57mg/mL(99.36mM;Needultrasonicandwarming)DMSO:57mg/mL(99.36mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.7431mL8.7157mL17.4313mL5mM0.3486mL1.7431mL3.4863mL10mM0.1743mL0.8716mL1.7431mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。BIOLOGICALACTIVITY?物活性NDT9513727?種?效的，選擇性的，具有?服活性的，競爭性的?C5aR反向激動劑，其IC50值為11.6nM。NDT9513727可?于?炎癥疾病的研究[1]。IC50&TargetIC50:11.6nM(humanC5aR)[1]體外研究NDT9513727inhibitsC5a-stimulatedresponses,includingguanosine5'-3-O-(thio)triphosphatebinding,Ca2+mobilization,oxidativeburst,degranulation,cellsurfaceCD11bexpressionandchemotaxisinvariouscell1/3typeswithIC50sfrom1.1to9.2nM,respectively[1].體內(nèi)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)只為有資質(zhì)的科研機(jī)構(gòu)、醫(yī)藥企業(yè)