Icenticaftor-QBW251-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEIcenticaftorCat.No.:HY-109177CASNo.:1334546-77-8Synonyms:QBW251分?式:C??H??F?N?O?分?量:361.24作?靶點:CFTR作?通路:MembraneTransporter/IonChannel儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:150mg/mL(415.24mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.7682mL13.8412mL27.6824mL5mM0.5536mL2.7682mL5.5365mL10mM0.2768mL1.3841mL2.7682mL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；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:4.25mg/mL(11.77mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥4.25mg/mL(11.77mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥4.25mg/mL(11.77mM);ClearsolutionBIOLOGICALACTIVITY?物活性Icenticaftor(QBW251)?種具有?服活性CFTR通道增強劑，F(xiàn)508del和G551DCFTR的EC50分別為79nM和497nM。Icenticaftor可?于慢性阻塞性肺疾病(COPD)和囊性纖維化研究。IC50&TargetEC50:79nM(F508delCFTR)and497nM(G551DCFTR)[1]體外研究Icenticaftor(QBW251),anorallybioavailablesmallmoleculeCFTRpotentiator,canrestoreCFTRfunctioninspecificCFTRgenotypesaswellaswild-typeCFTR[2].體內(nèi)研究InSprague-Dawleyrats,thepharmacokineticprofileofIcenticaftorisestablished.Afteroraladministrationatadoseof3mg/kg,theoralbioavailabilityis90%,andAUClastis20?635nmol/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