LM22A-4-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELM22A-4Cat.No.:HY-100673CASNo.:37988-18-4分⼦式:C₁₅H₂₁N₃O₆分⼦量:339.34作⽤靶点:TrkReceptor作⽤通路:NeuronalSignaling;ProteinTyrosineKinase/RTK储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验H2O:≥50mg/mL(147.34mM)DMSO:≥29mg/mL(85.46mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.9469mL14.7345mL29.4690mL5mM0.5894mL2.9469mL5.8938mL10mM0.2947mL1.4734mL2.9469mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.37mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.37mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.37mM);Clearsolution4.请依序添加每种溶剂：PBSSolubility:120mg/mL(353.63mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性LM22A-4⼀种特异性的tyrosinekinasereceptorB激动剂，常⽤于神经系统疾病研究。体外研究LM22A-4significantlyup-regulatesOPNandALPasemRNAexpressioninadose-dependentmannerandOCmRNAlevelissignificantlyincreasedby5μMofLM22A-4.LM22A-4significantlyincreasesOPN,ALPaseandOCmRNAexpressioninatime-dependentmanner.LM22A-4stimulatedOPNandOCmRNAexpressioninHCEMcellsculturedwithmineralizingmedia[2].体内研究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—您⾝边的抑制剂⼤师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