HS-276-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEHS-276Cat.No.:HY-147141CASNo.:2767422-72-8分⼦式:C₂₄H₂₉N₅O₂分⼦量:419.52作⽤靶点:IRAK;TNFReceptor作⽤通路:Immunology/Inflammation;Apoptosis储存⽅式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(119.18mM;ultrasonicandwarmingandadjustpHto2withHClandheatto80°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3837mL11.9184mL23.8368mL5mM0.4767mL2.3837mL4.7674mL10mM0.2384mL1.1918mL2.3837mL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(5.96mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(5.96mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性HS-276⼀种⼝服有效且⾼选择性的TAK1抑制剂，Ki值为2.5nM。HS-276对TAK1、CLK2、GCK、ULK2、MAP4K5、IRAK1、NUAK、CSNK1G2、CAMKKβ-1和MLK1具有显著抑制作⽤，IC50值分别为8.25、29、33、63、125、264、270、810、1280和5585nM。HS-276可⽤于类风湿关节炎(RA)研究[1]。IC50&TargetIRAK1IRAK4264nM(IC50)2500nM(IC50)体外研究HS-276reducesexpressionofTNF,IL-6,andIL-1βinadose-dependentmanner,withIC50valuesof138,201,and234nM,respectively[1].体内研究HS-276(CIAmousemodelofinflammatoryarthritis,50mg/kg,IP,dailyfor6days)reducesinflammation,pannus,cartilagedamage(CD),boneresorption(BR),andperiostealboneformation(PBF)histologicalmanifestations[1].HS-276(CD-1mice,30mg/kg,Oralgavage,once)showsexcellentbioavailabilityinmicewithaCmaxof3.68μMand%Fof98.1%[1].REFERENCES[1].ScarneoS,etal.DevelopmentandEfficacyofanOrallyBioavailableSelectiveTAK1InhibitorfortheTreatmentofInflammatoryArthritis.ACSChemBiol.2022Mar18;17(3):536-544.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.