Ivacaftor-13C6-VX-770-sup-13-sup-C-sub-6-sub-生命科學試劑-MCEVIP

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEIvacaftor-13C6Cat.No.:HY-13017S4Synonyms:VX-770-13C6分?式:C????C?H??N?O?分?量:424.48作?靶點:Isotope-LabeledCompounds;CFTR;Autophagy作?通路:Others;MembraneTransporter/IonChannel;Autophagy儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Ivacaftor-13C6(VX-770-13C6)13C標記的Ivacaftor.Ivacaftor(VX-770)?種有效可?服的CFTR增效劑，靶向G551D-CFTR和F508del-CFTR的EC50分別為100nM和25nM。體外研究Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattentionbecauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs.REFERENCES[1].RussakEM,etal.ImpactofDeuteriumSubstitutiononthePharmacokineticsofPharmaceuticals.AnnPharmacother.2019;53(2):211-216.[2].DelaunayJL,etal.Functionaldefectofvariantsintheadenosinetriphosphate-bindingsitesofABCB4andtheirrescuebythecysticfibrosistransmembraneconductanceregulatorpotentiator,ivacaftor(VX-770).Hepatology.2017Feb;65(2):560-570[3].MutyamV,etal.TherapeuticbenefitobservedwiththeCFTRpotentiator,ivacaftor,inaCFpatienthomozygousfortheW1282XCFTRnonsensemutation.JCystFibros.2017Jan;16(1):24-29[4].HadidaS,etal.DiscoveryofN-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide(VX-770,ivacaftor),apotentandorallybioavailableCFTRpotentiator.JMedChem.2014Dec11;57(23):9776-9[5].VanGoorF,etal.RescueofCFairwayepithelialcellfunctioninvitrobyaCFTRpotentiator,VX-770.ProcNatlAcadSciUSA.2009Nov3;106(44):18825-30.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-379