Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEML133hydrochlorideCat.No.:HY-100230ACASNo.:1222781-70-5分?式:C??H??ClNO分?量:313.82作?靶點(diǎn):PotassiumChannel作?通路:MembraneTransporter/IonChannel儲(chǔ)存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(318.65mM;ultrasonicandwarmingandheatto60°C)H2O:<0.1mg/mL(insoluble)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.1865mL15.9327mL31.8654mL5mM0.6373mL3.1865mL6.3731mL10mM0.3187mL1.5933mL3.1865mL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(sealedstorage,awayfrommoisture)。-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%salineSolubility:≥2.08mg/mL(6.63mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(6.63mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.63mM);ClearsolutionBIOLOGICALACTIVITY?物活性ML133hydrochloride?個(gè)選擇性的Kir2家族通道的抑制劑，在pH7.4和pH8.5時(shí)的IC50值分別為1.8μM和290nM。IC50&TargetIC50:1.8μM(Kir2atpH7.4),290nM(Kir2atpH8.5)[1].體外研究ML133,whichinhibitsKir2.1withIC50of1.8μMatpH7.4and290nMatpH8.5,butexhibitslittleselectivityagainstothermembersofKir2.xfamilychannels[1].ML133hasnoeffectonKir1.1(IC50>300μM),anddisplaysweakactivityforKir4.1(76μM)andKir7.1(33μM),makingML133themostselectivesmallmoleculeinhibitoroftheKirfamilyreportedtodate[1].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?CellMetab.2022Sep7;S1550-4131(22)00359-X.?PharmacolRes.2022Feb2;177:106112.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].WangHR,etal.SelectiveinhibitionoftheK(ir)2familyofinwardrectifierpotassiumchannelsbyasmallmoleculeprobe:thediscovery,SAR,andpharmacologicalcharacterizationofML133.ACSChemBiol.2011Aug19;6(8):845-56.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch