Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEST034307Cat.No.:HY-101279CASNo.:133406-29-8分?式:C??H?Cl?O?分?量:297.95作?靶點:AdenylateCyclase作?通路:GPCR/GProtein儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:16.67mg/mL(55.95mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.3563mL16.7813mL33.5627mL5mM0.6713mL3.3563mL6.7125mL10mM0.3356mL1.6781mL3.3563mL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%salineSolubility:≥1.67mg/mL(5.60mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥1.67mg/mL(5.60mM);ClearsolutionBIOLOGICALACTIVITY?物活性ST034307?種有效的，選擇性的adenylylcyclase1抑制劑，IC50值為2.3μM。IC50&TargetIC50:2.3μM(AC1)[1]體外研究ST034307revealsselectiveinhibitionofAC1andpotentiatesAC8activitytoanonsignificantsmallextent.ST034307potentiatesphorbol12-myristate13-acetate(PMA)-stimulatedcAMPproductionbyAC2.ST034307significantlyinhibitstheforskolin-orisoproterenol-stimulatedAC1activityinHEKcellsstablyexpressingAC1.Incontrast,ST034307hasnosignificanteffectsinthewild-typeHEKcells.ST034307significantlyinhibitstheCa2+/calmodulin-stimulatedcAMPaccumulationinthehippocampalhomogenates.ST034307dose-dependentlyinhibitsboththedevelopmentandthemaintenanceofMOR-mediatedsensitizationofAC1[1].體內研究ST034307(0.25μg)causesasignificantreliefofCFA-inducedinflammatorypaininmice.ST034307exhibitsanestimatedmedianeffectivedose(E50)valueforanalgesiaof0.28μginthemousepainmodel[1].PROTOCOLCellAssay[1]CellviabilityassaysareconductedwithHEK-AC1cellsfollowingplatingandcompoundincubationprotocolsidenticaltotheproceduresdescribedin“cAMPaccumulationincells.”Cellviabilityismeasuredasapercentageofvehicleusing2%TritonX-100asacontrol.TheCellTiter-GloLuminescentCellViabilityAssaykitfromPromegaisusedtoassesscellviabilityaccordingtothemanufacturer’sinstructions.LuminescencecountsaremeasuredusingSynergy4.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產品發表的科研?獻?NatCommun.2022Jul22;13(1):4255.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BrustTF,etal.Identificationofaselectivesmall-moleculeinhibitoroftype1adenylylcyclaseactivitywithanalgesicproperties.SciSignal.2017Feb21;10(467).McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedi