TAK-418-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETAK-418Cat.No.:HY-138830CASNo.:1818252-53-7分⼦式:C₁₇H₂₅ClN₂O₂S分⼦量:356.91作⽤靶点:HistoneDemethylase作⽤通路:Epigenetics储存⽅式:-20°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性数据体外实验DMSO:55mg/mL(154.10mM;ultrasonicandwarmingandheatto60°C)H2O:≥16.67mg/mL(46.71mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8018mL14.0091mL28.0183mL5mM0.5604mL2.8018mL5.6037mL10mM0.2802mL1.4009mL2.8018mL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(sealedstorage,awayfrommoistureandlight)。-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:≥5.5mg/mL(15.41mM);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:≥5.5mg/mL(15.41mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性TAK-418⼀种选择性的，具有⼝服活性的LSD1(KDM1A)酶抑制剂，IC50为2.9nM。TAK-418在神经发育障碍模型中解除异常的表观遗传机制并改孤独症症状。体内研究TAK-418(1mg/kg;p.o.;oncedailyfor14days)amelioratessomeautismspectrumdisorder(ASD)-likebehaviorsinneurodevelopmentaldisordermodelrodents[1].TAK-418increasesH3K4me1/2/3andH3K9me2levelsattheUcp2geneandinducedUcp2mRNAexpressioninprimaryculturedratneurons.TAK-418alsoincreasesH3K4me1/2/3attheBdnfgene.TAK-418avoidsthestericinterferencewithGFI1Binthebindingpocketthroughthegenerationofacompactformylatedadductformofcoenzymeflavinadeninedinucleotide(FAD).TAK-418showsagoodpharmacokineticprofileinrodentsandinhibitsLSD1enzymeactivityinthebrainwithoutcausinghematologicaltoxicityinrodents[1].SingleadministrationofTAK-418at1or3mg/kgincreasesH3K4me2levelsatUcp2geneinthemousebrain[1].TAK-418canameliorateneurologicalproblemsatthecellular,molecular,geneexpression,andfunctionallevelsinamousemodelofKS(Kmt2d+/βGeomice)[2].REFERENCES[1].BabaR,etal.LSD1enzymeinhibitorTAK-418unlocksaberrantepigeneticmachineryandimprovesautismsymptomsinneurodevelopmentaldisordermodels.SciAdv.2021;7(11):eaba1187.Published2021Mar12.[2].ZhangL,etal.InhibitionofKDM1AactivityrestoresadultneurogenesisandimproveshippocampalmemoryinamousemodelofKabukisyndrome.MolTherMethodsClinDev.2021;20:779-791.Published2021Feb18McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicala