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(diǎn):AdenylateCyclase作?通路:GPCR/GProtein儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)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(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(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(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?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，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:≥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(nèi)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(chǎn)品發(fā)表的科研?獻(xiàn)?NatCommun.2022Jul22;13(1):4255.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BrustTF,etal.Identificationofaselectivesmall-moleculeinhibitoroftype1adenylylcyclaseactivitywithanalgesicproperties.SciSignal.2017Feb21;10(467).McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedi