Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEML213Cat.No.:HY-101843CASNo.:489402-47-3分?式:C??H??NO分?量:257.37作?靶點:PotassiumChannel作?通路:MembraneTransporter/IonChannel儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:36.67mg/mL(142.48mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.8855mL19.4273mL38.8546mL5mM0.7771mL3.8855mL7.7709mL10mM0.3885mL1.9427mL3.8855mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)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(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?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(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)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(xiàn)沉淀、析出現(xiàn)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%salineSolubility:≥2.75mg/mL(10.69mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.75mg/mL(10.69mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.75mg/mL(10.69mM);ClearsolutionBIOLOGICALACTIVITY?物活性ML213?種具有選擇性的Kv7.2和Kv7.4通道增強劑，EC50值分別為230nM和510nM。IC50&TargetEC50:230nM(Kv7.2channel),510nM(Kv7.4channel)[2][3]體外研究ML213(100nM-30μM)increasesmaximalconductancetoapeakat212%±27%ofcontrol,withanEC50of0.8±0.3μM.ML213(10μM)reducesthedeactivationratesofKv7.4currentsby4.6-foldinthevoltagerangefrom?130mVto?90mV.ML213isapotentandeffectiveactivatorofhomomericKv7.5channelsoverexpressedinA7r5cells.ML213increasesmaximalconductanceofKv7.5channelswithanEC50of0.7±0.2μM.ML213(10μM)alsoreducesdeactivationratesofKv7.5currentsby5.9-foldonaverage.ML213producessimilareffectsonheteromericKv7.4/7.5channels:204%±11%maximalincreaseinconductancewithanEC50of1.1±0.6μManda34.2±3.3mVmaximalnegativeshiftoftheactivationcurve,withanEC50of3.8±1.2μM[1].ML213causesavasorelaxationindifferentprecontractedratbloodvessels.ML213(10μM)alsohyperpolarizesmesentericarterysmoothmusclecells[2].ML213causesaconcentration-dependentshiftintheV1/2forKCNQ2activationwithanEC50340±70nMandamaximalshiftof37.4mV[3].REFERENCES[1].BrueggemannLI,etal.DifferentialactivationofvascularsmoothmuscleKv7.4,Kv7.5,andKv7.4/7.5channelsbyML213andICA-069673.MolPharmacol.2014Sep;86(3):330-41.[2].JeppsTA,etal.VasorelaxanteffectsofnovelKv7.4channelenhancersML213andNS15370.BrJPharmacol.2014Oct;171(19):4413-24.[3].YuH,etal.Discovery,Synthesis,andStructureActivityRelationshipofaSeriesofN-Aryl-bicyclo[2.2.1]heptane-2-carboxamides:CharacterizationofML213asaNovelKCNQ2andKCNQ4PotassiumChannelOpener.ACSChemNeurosci.2011Oct19;2(10):572-577McePdfHeightCaution:Producthasnotbeenfullyvalidatedform