Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEIK1inhibitorPA-6Cat.No.:HY-112544CASNo.:500715-03-7Synonyms:PA-6分?式:C??H??N?O?分?量:492.61作?靶點:PotassiumChannel作?通路:MembraneTransporter/IonChannel儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:125mg/mL(253.75mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.0300mL10.1500mL20.3000mL5mM0.4060mL2.0300mL4.0600mL10mM0.2030mL1.0150mL2.0300mL請根據產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，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?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：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；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沉淀、析出現象，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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(4.22mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.22mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.22mM);ClearsolutionBIOLOGICALACTIVITY?物活性IK1inhibitorPA-6(PA-6)?種噴他脒類似物，有效的、選擇性的IK1(KIR2.x離?通道攜帶向內整流電流)抑制劑，?和??中對KIR2.x電流的IC50值為12-15nM。IK1inhibitorPA-6(PA-6)可上調KIR2.1的蛋?表達，誘導細胞內KIR2.1的蛋?的積累。IK1inhibitorPA-6(PA-6)有研究房顫和?律失常的潛?。IC50&TargetIC50:12-15nM(KIR2.xcurrents)[1].戶使?本產品發表的科研?獻?NatCommun.2022Jun21;13(1):3544.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].TakanariH,etal.EfficientandspecificcardiacIK?inhibitionbyanewpentamidineanalogue.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