Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENS5806Cat.No.:HY-108588CASNo.:426834-69-7分?式:C??H?Br?F?N?O分?量:574.07作?靶點:PotassiumChannel作?通路:MembraneTransporter/IonChannel儲存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:250mg/mL(435.49mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.7419mL8.7097mL17.4195mL5mM0.3484mL1.7419mL3.4839mL10mM0.1742mL0.8710mL1.7419mL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(fù)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(dāng)?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(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?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>>90%cornoilSolubility:≥2.08mg/mL(3.62mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性NS5806?種有效的鉀電流激活劑，可增加KV4.3/KChIP2峰值電流幅度，EC50為5.3μM。NS5806會在包含KChIP2的通道復(fù)合體中降低KV4.3和KV4.2電流衰減。IC50&TargetIC50:5.3nM(KV4.3)[1]體外研究NS5806(10μM)inducesa65%increaseofKV4.3/KChIP2/DPP6peakcurrentamplitudesconcentration-dependentlyandthetimecourseofinactivation(τ)isslowedwithanEC50valueof25.4μMinCHO-K1cells[1].NS5806activatescaninetransientoutwardpotassiumcurrent(Ito)withanIC50of40.7nMandanEC50of1.6nMforinhibitionandstimulationonrabbit,respectively[2].NS5806(10-100nM)hasconcentration-dependenteffectsonventricularandatrialIto[2].REFERENCES[1].ChengH,etal.Differentialresponsesofrabbitventricularandatrialtransientoutwardcurrent(Ito)totheItomodulatorNS5806.PhysiolRep.2017Mar;5(5).pii:e13172.[2].LundbyA,etal.EffectoftheI(to)activatorNS5806onclonedK4channelsdependsontheaccessoryproteinKChIP2.BrJPharmacol.2010Aug;160(8):2028-44.doi:10.1111/j.1476-5381.2010.00859.x.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:4