PAP-1-5-4-Phenoxybutoxy-psoralen-DataSheet-生命科学试剂-MedChemExpressVIP

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPAP-1Cat.No.:HY-10015CASNo.:870653-45-5Synonyms:5-(4-Phenoxybutoxy)psoralen分⼦式:C₂₁H₁₈O₅分⼦量:350.36作⽤靶点:PotassiumChannel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(142.71mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8542mL14.2710mL28.5421mL5mM0.5708mL2.8542mL5.7084mL10mM0.2854mL1.4271mL2.8542mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(7.14mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(7.14mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.14mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性PAP-1(5-(4-Phenoxybutoxy)psoralen)⼀种有效的，选择性的，⼝服活性的Kv1.3阻滞剂(EC50=2nM)。PAP-1以使⽤依赖性⽅式阻⽌Kv1.3，并通过优先绑定到通道的C型灭活状态来起作⽤。PAP-1⽐Kv1.5(EC50=45nM)表现出23倍的选择性，并且⽐所有其他Kv1家族通道表现出33到125倍的选择性。PAP-1不表现出细胞毒性或光毒性作⽤。IC50&TargetEC50:2nM(Kv1.3),45nM(Kv1.5)[1]体外研究PAP-1(2-100nM;30minutes)suppressestheproliferationofCCR7-TEMcellswithIC50of10nM[1].CellProliferationAssay[1]CellLine:CCR7-TEMcells(anti-CD3Abstimulated)Concentration:2,10,25,100nMIncubationTime:30minutesResult:SuppressestheProliferationofCCR7-TEMcellswithIC50of10nM.体内研究PAP-1(0.3-3mg/kg;i.p.;threetimesdailyfor48hours)preventsdelayedtypehypersensitivity(DTH)inlewisrats[1].AnimalModel:9-to11-week-oldfemaleLewisrats[1]Dosage:Intraperitonealinjection;threetimesdailyfor48hoursAdministration:0.3,1,3mg/kgResult:Dose-dependentlysuppressedtheDTHreaction.户使⽤本产品发表的科研⽂献•CellMolImmunol.2020Mar;17(3):283-299.•NatCommun.2022Jun21;13(1):3544.•IntJMolSci.2022Oct19;23(20):12565.•FASEBJ.2021Feb;35(2):e20995.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•ExpNeurol.2020Oct;332:113399.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SchmitzA,etal.DesignofPAP-1,aselectivesmallmoleculeKv1.3blocker,forthesuppressionofeffectormemoryTcellsinautoimmunediseases.MolPharmacol.2005Nov;68(5):1254-70.[2].PereiraLE,etal.Pharmacokinetics,toxicity,andfunctionalstudiesoftheselectiveKv1.3channelblocker5-(4-phenoxybutoxy)psoraleninrhesusmacaques.ExpBiolMed(Maywood).2007Nov;232(10):1338-54.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedi