THK5351-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETHK5351Cat.No.:HY-101183CASNo.:1707147-26-9分⼦式:C₁₈H₁₈FN₃O₂分⼦量:327.35作⽤靶点:TauProtein作⽤通路:NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(152.74mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.0548mL15.2742mL30.5483mL5mM0.6110mL3.0548mL6.1097mL10mM0.3055mL1.5274mL3.0548mL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:≥2.5mg/mL(7.64mM);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%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.64mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.64mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性THK5351被放射性标记后可作为放射性⽰踪剂，⽤于研究⼤脑中tau病理成像。体外研究AggregatedtauproteinisamajorneuropathologicalsubstratecentraltothepathophysiologyofneurodegenerativediseasessuchasAlzheimer'sdisease(AD).18F-THK5351bindstoAlzheimerdiseasehippocampalhomogenateswithhighaffinity(Kd=2.9nM;maximumnumberofbindingsites=368.3pmol/gtissue).Ithasfastdissociationfromwhite-mattertissue.TheTHK5351bindingamountcorrelateswiththeamountoftaudepositsintissue[1].体内研究THK5351exhibitsfavorablepharmacokineticsandnodefluorinationinmice.18F-THK5351entersthebrainimmediatelyafterintravenousinjectionandshowsafastwashoutfromthebrain.At0.1and1mg/kg,noanimalsdiedandnotreatment-relatedchangesinanyanimalarenotedinclinicalobservations,bodyweightmeasurement,andpathologicexamination[1].AutoradiographyinthebrainsectionsofpatientswithPSPdemonstrates[3H]THK-5351bindingtotaudepositswithahighselectivity.AlthoughpatientswithPSPexhibitsnoremarkable[18F]THK-5351retentioninthetemporalcortex,significantlyhighertracerretentionisobservedintheglobuspallidusandmidbrain[2].REFERENCES[1].HaradaR,etal.18F-THK5351:ANovelPETRadiotracerforImagingNeurofibrillaryPathologyinAlzheimerDisease.JNuclMed.2016Feb;57(2):208-14.[2].IshikiA,etal.Tauimagingwith[18F]THK-5351inprogressivesupranuclearpalsy.EurJNeurol.2017Jan;24(1):130-136.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicati