Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPAP-1Cat.No.:HY-10015CASNo.:870653-45-5Synonyms:5-(4-Phenoxybutoxy)psoralen分?式:C??H??O?分?量:350.36作?靶點(diǎn):PotassiumChannel作?通路:MembraneTransporter/IonChannel儲(chǔ)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(142.71mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.8542mL14.2710mL28.5421mL5mM0.5708mL2.8542mL5.7084mL10mM0.2854mL1.4271mL2.8542mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)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(qǐng)先按照InVitro?式配制澄的儲(chǔ)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(chǔ)備液可以根據(jù)儲(chǔ)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(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(7.14mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(7.14mM);Suspendedsolution;Needultrasonic3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.14mM);ClearsolutionBIOLOGICALACTIVITY?物活性PAP-1(5-(4-Phenoxybutoxy)psoralen)?種有效的，選擇性的，?服活性的Kv1.3阻滯劑(EC50=2nM)。PAP-1以使?依賴性?式阻?Kv1.3，并通過優(yōu)先綁定到通道的C型滅活狀態(tài)來起作?。PAP-1?Kv1.5(EC50=45nM)表現(xiàn)出23倍的選擇性，并且?所有其他Kv1家族通道表現(xiàn)出33到125倍的選擇性。PAP-1不表現(xiàn)出細(xì)胞毒性或光毒性作?。IC50&TargetEC50:2nM(Kv1.3),45nM(Kv1.5)[1]體外研究PAP-1(2-100nM;30minutes)suppressestheproliferationofCCR7-TEMcellswithIC50of10nM[1].CellProliferationAssay[1]CellLine:CCR7-TEMcells(anti-CD3Abstimulated)Concentration:2,10,25,100nMIncubationTime:30minutesResult:SuppressestheProliferationofCCR7-TEMcellswithIC50of10nM.體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?CellMolImmunol.2020Mar;17(3):283-299.?NatCommun.2022Jun21;13(1):3544.?IntJMolSci.2022Oct19;23(20):12565.?FASEBJ.2021Feb;35(2):e20995.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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