Icenticaftor-QBW251-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEIcenticaftorCat.No.:HY-109177CASNo.:1334546-77-8Synonyms:QBW251分⼦式:C₁₂H₁₃F₆N₃O₃分⼦量:361.24作⽤靶点:CFTR作⽤通路:MembraneTransporter/IonChannel储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:150mg/mL(415.24mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7682mL13.8412mL27.6824mL5mM0.5536mL2.7682mL5.5365mL10mM0.2768mL1.3841mL2.7682mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:4.25mg/mL(11.77mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥4.25mg/mL(11.77mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥4.25mg/mL(11.77mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Icenticaftor(QBW251)⼀种具有⼝服活性CFTR通道增强剂，F508del和G551DCFTR的EC50分别为79nM和497nM。Icenticaftor可⽤于慢性阻塞性肺疾病(COPD)和囊性纤维化研究。IC50&TargetEC50:79nM(F508delCFTR)and497nM(G551DCFTR)[1]体外研究Icenticaftor(QBW251),anorallybioavailablesmallmoleculeCFTRpotentiator,canrestoreCFTRfunctioninspecificCFTRgenotypesaswellaswild-typeCFTR[2].体内研究InSprague-Dawleyrats,thepharmacokineticprofileofIcenticaftorisestablished.Afteroraladministrationatadoseof3mg/kg,theoralbioavailabilityis90%,andAUClastis20ꢀ635nmol/L•h[1].REFERENCES[1].DarrenLeGrand,etal.DiscoveryofIcenticaftor(QBW251),aCysticFibrosisTransmembraneConductanceRegulatorPotentiatorwithClinicalEfficacyinCysticFibrosisandChronicObstructivePulmonaryDisease.JMedChem.2021Jun10;64(11):7241-7260.[2].StevenMRowe,etal.EfficacyandSafetyoftheCFTRPotentiatorIcenticaftor(QBW251)inCOPD:ResultsfromaPhase2RandomizedTrial.IntJChronObstructPulmonDis.2020Oct5;15:2399-2409.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch