CFTR-inh-172-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECFTR(inh)-172Cat.No.:HY-16671CASNo.:307510-92-5分?式:C??H??F?NO?S?分?量:409.4作?靶點(diǎn):CFTR;Autophagy作?通路:MembraneTransporter/IonChannel;Autophagy儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:50mg/mL(122.13mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4426mL12.2130mL24.4260mL5mM0.4885mL2.4426mL4.8852mL10mM0.2443mL1.2213mL2.4426mL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(fù)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(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?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(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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%salineSolubility:2.5mg/mL(6.11mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.11mM);ClearsolutionBIOLOGICALACTIVITY?物活性CFTR(inh)-172?效選擇性的CFTR通道阻斷劑;在2分鐘內(nèi)可逆地抑制CFTR短路電流的Ki值為300nM。IC50&TargetKi:300nM(CFTR)[1]體外研究InhibitionbyCFTR(inh)-172iscompleteinapproximately10minutes(t1/2=4minutes)andisreversedafterishoutwitht1/2approximately5minutes.CFTRinh-172isnontoxictoFRTcellsafter24hoursatconcentrationsupto100μM[1].CFTR(inh)-172doesnotalterCFTRunitaryconductance(8pS),butreducesopenprobabilityby>90%withKi=0.6μM.Thiseffectisduetoincreasedmeanchannelclosedtimewithoutchangingmeanchannelopentime.TheKivaluesforinhibitionofCl-currentinwild-type,G551D,andG1349DCFTRareabout0.5μM;however,Kiissignificantlyreducedto0.2μMforvF508CFTR[2].體內(nèi)研究AsingleintraperitonealinjectionofCFTR(inh)-172(250μg/kg)inmicereducesbymorethan90%choleratoxin–inducedfluidsecretioninthesmallintestineover6hours.CFTR(inh)-172isnontoxicathighconcentrationsinmousemodels.CFTRinh-172significantlyreducesfluidsecretiontothatinsalinecontrolloops,whereasaninactiveCFTRinh-172analogdoesnotinhibitfluidsecretion[1].PROTOCOLCellAssay[1]CFTR(inh)-172isdilutedinDMSOasa10mMstocksolutionanddilutedwithappropriatemedium.Fischerratthyroid(FRT)cellscoexpressinghumanwild-typeCFTRandthehalideindicatorYFP-H148Qaregenerated.Celltoxicityisassayedbythedihydrorhodaminemethodat24hoursaftercellincubationwith0–1,000μMinhibitorCFTR(inh)-172[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:Animaltoxicityisassessedbymeasurementofserumchemistriesandhematologyinmiceat5daysAdministration[1]afterdailyintraperitonealinjectionswith0-1,000μg/kgCFTR(inh)-172[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?CellStemCell.2019Sep5;25(3):373-387.e9.?PLoSBiol.2021Feb16;19(2):e3001090.?IntJMolSci.2022Feb23;23(5):2442.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].MaT,etal.ThiazolidinoneCFTRinhibitoridentifiedbyhigh-throughputscreeningblockscholeratoxin-inducedintestinalfluidsecretion.JClinInvest.2002Dec;110(11):1651-8.[2].TaddeiA,etal.AlteredchannelgatingmechanismforCFTRinhibitionbyahigh-affinitythiazolidinoneblocker.FEBSLett.2004Jan30;558(1-3):52-6.McePdfHeightCaution:Producth