THK5351-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETHK5351Cat.No.:HY-101183CASNo.:1707147-26-9分?式:C??H??FN?O?分?量:327.35作?靶點:TauProtein作?通路:NeuronalSignaling儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:50mg/mL(152.74mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.0548mL15.2742mL30.5483mL5mM0.6110mL3.0548mL6.1097mL10mM0.3055mL1.5274mL3.0548mL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?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據(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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.64mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.64mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.64mM);ClearsolutionBIOLOGICALACTIVITY?物活性THK5351被放射性標記后可作為放射性?蹤劑，?于研究?腦中tau病理成像。體外研究AggregatedtauproteinisamajorneuropathologicalsubstratecentraltothepathophysiologyofneurodegenerativediseasessuchasAlzheimer'sdisease(AD).18F-THK5351bindstoAlzheimerdiseasehippocampalhomogenateswithhighaffinity(Kd=2.9nM;maximumnumberofbindingsites=368.3pmol/gtissue).Ithasfastdissociationfromwhite-mattertissue.TheTHK5351bindingamountcorrelateswiththeamountoftaudepositsintissue[1].體內研究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