2-6-Dichloro-N-2-cyclopropanecarboxamido-pyridin-4-yl-benzamide-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamideCat.No.:HY-120469CASNo.:1258292-64-6分⼦式:C₁₆H₁₃Cl₂N₃O₂分⼦量:350.2作⽤靶点:JAK作⽤通路:Epigenetics;JAK/STATSignaling;StemCell/Wnt储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:62.5mg/mL(178.47mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8555mL14.2776mL28.5551mL5mM0.5711mL2.8555mL5.7110mL10mM0.2856mL1.4278mL2.8555mL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(protectfromlight)。-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:≥2.08mg/mL(5.94mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.94mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性GDC-046⼀种有效的，具有⼝服活性的选择性TYK2抑制剂，对TYK2，JAK1，JAK2和JAK3的Ki分别为4.8、0.7、0.7和0.4nM[1]。IC50&TargetTyk2JAK1JAK2JAK34.8nM(Ki)0.7nM(Ki)0.7nM(Ki)0.4nM(Ki)体外研究Incell-basedassays,GDC-046demonstratesreasonablepotencyinblockingtheIL-12pathway(IL-12pSTAT4EC50=380nM)whiledisplayinglessactivityintheEPO(JAK2)pathway(EPOpSTAT5EC50=1700nM)andIL-6(JAK1)pathway(IL-6pSTAT3EC50=2000nM)[1].体内研究Inmice,GDC-046exhibitsrelativelyhighclearance(65mL/min/kg)whendosedintravenously(i.v.1mg/kg)andexhibitsmodestoralexposure(AUC=2.6μM·hatp.o.5mg/kg)[1].REFERENCES[1].JunLiang,etal.LeadOptimizationofa4-aminopyridineBenzamideScaffoldtoIdentifyPotent,Selective,andOrallyBioavailableTYK2Inhibitors.JMedChem.2013Jun13;56(11):4521-36.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel: