ST034307-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEST034307Cat.No.:HY-101279CASNo.:133406-29-8分⼦式:C₁₀H₄Cl₄O₂分⼦量:297.95作⽤靶点:AdenylateCyclase作⽤通路:GPCR/GProtein储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:16.67mg/mL(55.95mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.3563mL16.7813mL33.5627mL5mM0.6713mL3.3563mL6.7125mL10mM0.3356mL1.6781mL3.3563mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥1.67mg/mL(5.60mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥1.67mg/mL(5.60mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性ST034307⼀种有效的，选择性的adenylylcyclase1抑制剂，IC50值为2.3μM。IC50&TargetIC50:2.3μM(AC1)[1]体外研究ST034307revealsselectiveinhibitionofAC1andpotentiatesAC8activitytoanonsignificantsmallextent.ST034307potentiatesphorbol12-myristate13-acetate(PMA)-stimulatedcAMPproductionbyAC2.ST034307significantlyinhibitstheforskolin-orisoproterenol-stimulatedAC1activityinHEKcellsstablyexpressingAC1.Incontrast,ST034307hasnosignificanteffectsinthewild-typeHEKcells.ST034307significantlyinhibitstheCa2+/calmodulin-stimulatedcAMPaccumulationinthehippocampalhomogenates.ST034307dose-dependentlyinhibitsboththedevelopmentandthemaintenanceofMOR-mediatedsensitizationofAC1[1].体内研究ST034307(0.25μg)causesasignificantreliefofCFA-inducedinflammatorypaininmice.ST034307exhibitsanestimatedmedianeffectivedose(E50)valueforanalgesiaof0.28μginthemousepainmodel[1].PROTOCOLCellAssay[1]CellviabilityassaysareconductedwithHEK-AC1cellsfollowingplatingandcompoundincubationprotocolsidenticaltotheproceduresdescribedin“cAMPaccumulationincells.”Cellviabilityismeasuredasapercentageofvehicleusing2%TritonX-100asacontrol.TheCellTiter-GloLuminescentCellViabilityAssaykitfromPromegaisusedtoassesscellviabilityaccordingtothemanufacturer’sinstructions.LuminescencecountsaremeasuredusingSynergy4.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•NatCommun.2022Jul22;13(1):4255.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BrustTF,etal.Identificationofaselectivesmall-moleculeinhibitoroftype1adenylylcyclaseactivitywithanalgesicproperties.SciSignal.2017Feb21;10(467).McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedi