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(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:125mg/mL(253.75mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.0300mL10.1500mL20.3000mL5mM0.4060mL2.0300mL4.0600mL10mM0.2030mL1.0150mL2.0300mL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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(4.22mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.22mM);Clearsolution3.請(qǐng)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(lèi)似物，有效的、選擇性的IK1(KIR2.x離?通道攜帶向內(nèi)整流電流)抑制劑，?和??中對(duì)KIR2.x電流的IC50值為12-15nM。IK1inhibitorPA-6(PA-6)可上調(diào)KIR2.1的蛋?表達(dá)，誘導(dǎo)細(xì)胞內(nèi)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(hù)使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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