Galicaftor-ABBV-2222-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGalicaftorCat.No.:HY-111111CASNo.:1918143-53-9Synonyms:ABBV-2222;GLPG-2222分⼦式:C₂₈H₂₁F₄NO₇分⼦量:559.46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:50mg/mL(89.37mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7874mL8.9372mL17.8744mL5mM0.3575mL1.7874mL3.5749mL10mM0.1787mL0.8937mL1.7874mL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:≥2.5mg/mL(4.47mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.47mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Galicaftor(ABBV-2222;GLPG-2222)⼀种有效的，具有⼝服活性的囊性纤维化跨膜电导调节剂(CFTR)校正剂，可⽤于囊性纤维化的研究。体外研究Galicaftor(ABBV-2222;GLPG-2222)exhibitspotentinvitrofunctionalactivityinprimarypatientcellsharboringF508del/F508delCFTR,withanEC50[2].体内研究TheratpharmacokinetictestsareperformedonGalicaftor(ABBV-2222;GLPG-2222;1mg/kg,i.v.;1mg/kg,p.o.)toillustrateitspharmacokineticpropertiesinrats.TheT1/2is2.7hours(i.v.).Andforintragastricadministration,thebioavailability(%F)is74%[1].REFERENCES[1].XueqingWang,etal.Discoveryof4-[(2R,4R)-4-({[1-(2,2-Difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl}amino)-7-(difluoromethoxy)-3,4-dihydro-2H-chromen-2-yl]benzoicAcid(ABBV/GLPG-2222),aPotentCysticFibrosisTransmembraneConductanceRegulator[2].AshvaniKSingh,etal.BiologicalCharacterizationofF508delCFTRProteinProcessingbytheCFTRCorrectorABBV-2222/GLPG2222.JPharmacolExpTher.2020Jan;372(1):107-118.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Te