AS1810722-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrariesAS1810722Cat.No.:HY-134772CASNo.:909561-15-5分⼦式:C₂₅H₂₅F₂N₇O分⼦量:477.51作⽤靶点:STAT;CytochromeP450作⽤通路:JAK/STATSignaling;StemCell/Wnt;MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:62.5mg/mL(130.89mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0942mL10.4710mL20.9420mL5mM0.4188mL2.0942mL4.1884mL10mM0.2094mL1.0471mL2.0942mL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，并请注意储备液的保存⽅式和期限。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%DMSO90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(4.36mM);Suspendedsolution;Needultrasonic此⽅案可获得2.08mg/mL(4.36mM)的均匀悬浊液，悬浊液可⽤于⼝服和腹腔注射。以1mL⼯作液为例，取100μL20.8mg/mL的澄DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶液中，混合均匀。1/3BIOLOGICALACTIVITY⽣物活性AS1810722⼝服有效的STAT6抑制剂，IC50为1.9nM。AS1810722显⽰出良好的CYP3A4抑制作⽤。AS1810722⼀种稠合双环嘧啶衍⽣物，具有⽤于过敏性疾病，例如哮喘和特应性疾病研究的潜⼒。IC50&TargetSTAT6CYP3A41.9nM(IC50)体外研究AS1810722(compound24)inhibitsproductionofIL-4withanIC50of2.4nM,butshowsnoeffectonproductionofIFN-γ[1].体内研究AS1810722(compound24;0.03-0.3mg/kg;orally;30minbefore,and24hand48hafterOVAexposure)suppresseosinophilinfiltrationinthelunginadose-dependentmannerinanantigen-inducedmouseasthmaticmodel[1].AS1810722inhibitsinvitroTh2differentiationwithanIC50of2.4nMwithoutaffectingtype1helperT(Th1)celldifferentiationandeosinophilinfiltrationinanantigen-inducedmouseasthmaticmodelafteroraladministration[1].AnimalModel:FemaleBalb/cmiceasthmaticmodelbyintraperitonealinjectionofovalbumin(OVA)-containingaluminumhydroxidegel[1]Dosage:0.03-0.3mg/kgAdministration:Orally;30minbefore,and24and48hafterOVAexposureResult:Suppressedeosinophilinfiltrationinthelunginadose-dependentmanner.REFERENCES[1].ShinyaNagashima,etal.Novel7H-pyrrolo[2,3-d]pyrimidinederivativesaspotentandorallyactiveSTAT6inhibitors.BioorgMedChem.2009Oct1;17(19):6926-36.McePdfHeight2/3MedChemExpress(MCE)只为有资质的科研机构、医药企业基于