WAY-262611-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEWAY-262611Cat.No.:HY-11035CASNo.:1123231-07-1分⼦式:C₂₀H₂₂N₄分⼦量:318.42作⽤靶点:β-catenin作⽤通路:StemCell/Wnt储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥42mg/mL(131.90mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.1405mL15.7025mL31.4051mL5mM0.6281mL3.1405mL6.2810mL10mM0.3141mL1.5703mL3.1405mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥1.67mg/mL(5.24mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1.67mg/mL(5.24mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥1.67mg/mL(5.24mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性WAY-262611Wnt/β-联蛋⽩激动剂，可增加⾻形成速率，在TCF-荧光素酶测定实验中的EC50值为0.63μM。WAY-262611也Dkk1的抑制剂。IC50&TargetEC50:0.63μM(β-Catenin)[1]体外研究WAY-262611hasthemostpotentactivityintheprimaryassay,lowkinaseinhibitionpotential,andhighsolubility[1].体内研究WAY-262611hasexcellentpharmacokineticpropertiesandshowsadosedependentincreaseinthetrabecularboneformationrateinovariectomizedratsfollowingoraladministration.CalvariaefromwtmicetreatedwithWAY-262611showsstatisticallyincreasedBFR,whilesimilarlytreatedKOanimalsarenodifferentfromcontrol.ThisindicatesthatWAY-262611isactingviatheWntβ-cateninpathwayandmostlikelythroughinhibitionofDkk-1[1].PROTOCOLAnimalRats:WAY-262611isdissolvedinDMSOanddilutedwithsalineforiv(Rats).WAY-262611ispreparedinAdministration[1]0.5%methylcellulose/2%Tween-80forpoOVXrats14aretreatedorallywith5(po,vehicle=0.5%methylcellulose/2%Tween-80,qd,28days)atfourdoses.Trabecularboneformationrate(BFR)inthetibiaisestablishedinalldosegroupsattheendofthein-lifeportionofthestudy.Acleardoseresponseandactivityaslowas0.3mg/kg/dayareobserved[1].Mice:ToconfirmactivityviatheWntpathway,thecalvariaeofwildtype(wt)andDkk-1knockout(KO)micearetreatedwith5onceadayfor7days(DMSOsolution,scinjection).TheKOanimalsarenotexpectedtorespondbecauseoftheinherentinabilitytoinhibitamissingtargetprotein,whilewildtypeanimalswithfullyexpressedDkk-1areexpectedtoshowapharmacologicalresponse[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•NatBiotechnol.2020Sep;38(9):1087-1096.•IntJBiochemCellBiol.2020Apr;121:105703.•JCellSci.2019May16;132(10):jcs228478.•Bone.2022Jun7;116456.•EvidBasedComplementAlternatMed.2019May30;2019:9692350.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].PelletierJC,etal.(1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine:awinglessbeta-cateninagonistthatincreasesboneformationrate.JMedChem.2009Nov26;52(22):6962-5.[2].LEnochson,etal.GDF5reducesMMP13expressioninhumanchondrocytesviaDKK1mediatedcanonicalWntsignalinginhibition.OsteoarthritisCartilage.2014Apr;22(4):566-77.McePdfHeightCaution:Product