Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESQ22536Cat.No.:HY-100396CASNo.:17318-31-9分?式:C?H??N?O分?量:205.22作?靶點:AdenylateCyclase作?通路:GPCR/GProtein儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(487.28mM;Needultrasonic)H2O:55mg/mL(268.01mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM4.8728mL24.3641mL48.7282mL5mM0.9746mL4.8728mL9.7456mL10mM0.4873mL2.4364mL4.8728mL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>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(12.18mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(12.18mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(12.18mM);Clearsolution4.請依序添加每種溶劑：PBSSolubility:25mg/mL(121.82mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性SQ22536?種有效的腺苷酸環(huán)化酶(AC)抑制劑。IC50&Targetadenylatecyclase(AC)[1]體外研究SQ22536(SQ22,536)effectivelyinhibitstheeffectofforskolinwithrespectiveIC50valuesof5μM.PreincubationwithgradedconcentrationsofSQ22536revealsthatbothSQ22536effectivelyinhibitsPACAP-inducedreportergeneactivationwithapproximateIC50valueof5μM.SQ22536morepotentlyinhibitsforskolin-inducedElkactivation(IC50=10μM)than8-Br-cAMP-inducedElkactivation(IC50=170μM).Mostnotably,therearesubstantialdifferencesinthereportedpotenciesofSQ22536toinhibittheactivitiesofrecombinantAC5andAC6,withrespectiveIC50valuesof2μMand360μM.Atagreaterconcentration(500μM),SQ22536significantlyinhibitsneuriteelongationduetoeitherforskolinor8-Br-cAMP[1].PROTOCOLCellAssay[1]HEK293CRE-luc2PGloResponseluciferasereportercellsaretransducedwithretroviralvectorsexpressingratPAC1hopreceptors.Individualcelllinesareobtainedbylimitingdilutioncloning,andaclonalPAC1-expressinglineispropagatedandusedforCREluciferaseassays.Inbrief,HEK293CRE-luc2Pcellsareplatedin96-wellplates(10,000cellsin80μLmediaperwell)inassaymedia(DMEMsupplementedwith1%fetalbovineserum).Onedayafterplating,cellsaretreatedwithACinhibitors(10μLinassaymedia/well)for30minutes,followedbyagonists(10μLinassaymedia/well),andareincubatedfor4hours.Luciferaseactivityisdeterminedaftertheadditionof100μL/wellBright-GloLuciferaseAssayReagent.Luminescence(RLU)ismeasuredinaVictor3microtiterplatereaderafter2minutesofagitationatroomtemperature.CyclicAMPismeasuredinNS-1cells.Inbrief,NS-1cellsareseededandgrownovernightin96-wellplates.Thenextday,cellsarepretreatedfor20minutesinmediacontainingthephosphodiesteraseinhibitor3-isobutyl-1-methylxanthine(0.5mM)withorwithoutSQ22536.Afterpretreatmentwithinhibitors,cellsarestimulatedwithagonists,addedas10×solutions,foranadditional20minutes.IntracellularcAMPisthenassayedusingthecAMPBiotrakenzymeimmunoassaykitformeasurementofnonacetylatedcAMP[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?ProgNeurobiol.2021Mar22;102041.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?CellDeathDis.2020May26;11(5):394.?IntJMolSci.2022,23(20),12595.?IntJMolSci.2022Sep14;23(18):10709.?iScience.2021,102812.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].EmeryAC,etal.AnewsiteandmechanismofactionforthewidelyusedadenylatecyclaseinhibitorSQ22,536.MolPharmacol.2013Jan;83(1):95-105.McePdfHe