IK1-inhibitor-PA-6-PA-6-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEIK1inhibitorPA-6Cat.No.:HY-112544CASNo.:500715-03-7Synonyms:PA-6分⼦式:C₃₁H₃₂N₄O₂分⼦量:492.61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:125mg/mL(253.75mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0300mL10.1500mL20.3000mL5mM0.4060mL2.0300mL4.0600mL10mM0.2030mL1.0150mL2.0300mL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:≥2.08mg/mL(4.22mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.22mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.22mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性IK1inhibitorPA-6(PA-6)⼀种喷他脒类似物，有效的、选择性的IK1(KIR2.x离⼦通道携带向内整流电流)抑制剂，⼈和⽼⿏中对KIR2.x电流的IC50值为12-15nM。IK1inhibitorPA-6(PA-6)可上调KIR2.1的蛋⽩表达，诱导细胞内KIR2.1的蛋⽩的积累。IK1inhibitorPA-6(PA-6)有研究房颤和⼼律失常的潜⼒。IC50&TargetIC50:12-15nM(KIR2.xcurrents)[1].户使⽤本产品发表的科研⽂献•NatCommun.2022Jun21;13(1):3544.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].TakanariH,etal.EfficientandspecificcardiacIK₁inhibitionbyanewpentamidineanalogue.CardiovascRes.2013Jul1;99(1):203-14.[2].JiY,etal.TheinwardrectifiercurrentinhibitorPA-6terminatesatrialfibrillationanddoesnotcauseventriculararrhythmiasingoatanddogmodels.BrJPharmacol.2017Aug;174(15):2576-2590.[3].JiY,etal.PA-6inhibitsinwardrectifiercurrentscarriedbyV93IandD172Ngain-of-functionKIR2.1channels,butincreaseschannelproteinexpression.JBiomedSci.2017Jul15;24(1):44.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonl