Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELM22A-4Cat.No.:HY-100673CASNo.:37988-18-4分?式:C??H??N?O?分?量:339.34作?靶點:TrkReceptor作?通路:NeuronalSignaling;ProteinTyrosineKinase/RTK儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗H2O:≥50mg/mL(147.34mM)DMSO:≥29mg/mL(85.46mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.9469mL14.7345mL29.4690mL5mM0.5894mL2.9469mL5.8938mL10mM0.2947mL1.4734mL2.9469mL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?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，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)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(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.37mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.37mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.37mM);Clearsolution4.請依序添加每種溶劑：PBSSolubility:120mg/mL(353.63mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性LM22A-4?種特異性的tyrosinekinasereceptorB激動劑，常?于神經(jīng)系統(tǒng)疾病研究。體外研究LM22A-4significantlyup-regulatesOPNandALPasemRNAexpressioninadose-dependentmannerandOCmRNAlevelissignificantlyincreasedby5μMofLM22A-4.LM22A-4significantlyincreasesOPN,ALPaseandOCmRNAexpressioninatime-dependentmanner.LM22A-4stimulatedOPNandOCmRNAexpressioninHCEMcellsculturedwithmineralizingmedia[2].體內(nèi)研究LM22A-4(10mg/kg,i.p.)significantlyreducesthedegreeoftissueinjuryandapoptosis(TUNELstainingandcaspase-3andBcl-2expression)comparedwithvehicletreatedgroup.LM22A-4alsosignificantlyamelioratestherecoveryoflimbfunction.LM22A-4(10mg/kg)treatmentresultsinasignificantincreaseinneuronnumber.LM22A-4administration(10mg/kg)significantlyimprovestheneurologicalscorescomparedwiththoseofthesolvent-treatedanimals[1].PROTOCOLAnimalICRmicearerandomlydividedintofivegroups:shamtreatment,spinalcordinjury,spinalcordinjuryAdministration[1]combinedwithsolventtreatment,spinalcordinjurycombinedwithLM22A-4treatment(10mg/kg),andspinalcordinjurycombinedwithLM22A-4treatment(15mg/kg),witheachgroupcontaining26animals.PreparationofthemouseSCImodelisbasedonapreviousstudyandonaprotocolemployedbythisgroup.Briefly,amouseisanesthetizedviatheadministrationofchloralhydrate(4mg/kg)beforea3-cmincisionisintroducedonitsback.T7-T11vertebraeareexposedunderasurgicalmicroscopebeforethelaminaeareremovedwithavascularcliptofullyexposethespinalcord.Thespinalcordisclampedwiththevascularclipfor1minutewithaforceof10g.Theanimalisthensubjectedtocompletestaunchingofthebleeding,andtheinciseddorsalmuscleandskinaresutured.Micefromthecontrolgroupundergolaminectomy,fullexposureofthespinalcord,andsubsequentsuturing,butwithoutaorticclamping.Afterthesurgery,themiceareplacedonawarmblanketuntilfullyawakeandarethenhousedincagesaccommodatinganormaldiet.AftertheSCItreatment,14micearesacrificedtoenablemolecularandhistologicalexaminations;theother14miceareallowedtolivefor20daysforneurologicalscoringandaresacrificedonday20viacervicaldislocation.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEREFERENCES[1].YuG,etal.ProtectiveeffectsofLM22A-4oninjuredspinalcordnerves.IntJClinExpPathol.2015Jun1;8(6):6526-32.eCollection2015.[2].KajiyaM,etal.BDNFmimeticcompoundLM22A-4regulatescementoblastdifferentiationviatheTrkB-ERK/Aktsignalingcascade.IntImmunopharmacol.2014Apr;19(2):245-52McePd