Upadacitinib-ABT-494-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEUpadacitinibCat.No.:HY-19569CASNo.:1310726-60-3Synonyms:ABT-494分⼦式:C₁₇H₁₉F₃N₆O分⼦量:380.37作⽤靶点:JAK作⽤通路:Epigenetics;JAK/STATSignaling;ProteinTyrosineKinase/RTK;StemCell/Wnt储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥22mg/mL(57.84mM)H2O:<0.1mg/mL(insoluble)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.6290mL13.1451mL26.2902mL5mM0.5258mL2.6290mL5.2580mL10mM0.2629mL1.3145mL2.6290mL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1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE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：1%DMSO>>99%salineSolubility:≥0.55mg/mL(1.45mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥1.67mg/mL(4.39mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1.67mg/mL(4.39mM);Clearsolution4.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥1.67mg/mL(4.39mM);Clearsolution5.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.75mg/mL(7.23mM);Clearsolution6.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.75mg/mL(7.23mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Upadacitinib(ABT-494)⼀种⾼效的、具有⼝服活性的、选择性Janus激酶1(JAK1)抑制剂(IC50=43nM)。Upadacitinib对JAK1的选择性约为JAK2(200nM）的74倍。Upadacitinib可⽤于多种⾃⾝免疫性疾病的研究。IC50&TargetJAK1JAK2JAK3Tyk20.043μM(IC50)0.2μM(IC50)2.3μM(IC50)4.7μM(IC50)体外研究Inbiochemicalassays,Upadacitinibis74-foldmoreselectiveforJAK-1thanforJAK-2(whichisinvolvedinerythropoiesis)and58-foldmoreselectiveforJAK-1thanforJAK-3(whichisinvolvedinimmunosurveillance)[1].TheenhancedselectivityofUpadacitinibforJAK-1overJAK-2andJAK-3mayofferanimprovedbenefit–riskprofileinpatientswithRArange[2].体内研究Upadacitinib(0.1-10mg/kg;oralgavage;twiceadayfor10days)demonstratesefficacyinratarthritismodels[3].AnimalModel:FemaleLewisrats(Ratadjuvant-inducedarthritismodel)[3]Dosage:0.1,0.3,1,3,10mg/kgAdministration:Oralgavage;twiceadayfor10daysResult:Inhibiteddiseasepathologyinratadjuvantinducedarthritis.户使⽤本产品发表的科研⽂献•AnnRheumDis.2021Jul;80(7):865-875.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•Biomedicines.2021,9(10),1413.•MolPharmacol.April5,2022.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].NakayamadaS,etal.RecentProgressinJAKInhibitorsfortheTreatmentofRheumatoidArthritis.BioDrugs.2016Oct;30(5):407-419.[2].J.Voss,etal.THU0127PharmacodynamicsofANovelJAK1SelectiveInhibitorinRatArthritisandAnemiaModelsandinHealthyHumanSubjects.doi10.1136/annrheumdis-2014-eular.3823.[3].ParmentierJM,etal.InvitroandinvivocharacterizationoftheJAK1selectivityofupadacitinib(ABT-494).BMCRheumatol.2018Aug28;2:23.McePdfHeightCaution:Producthasnotbeenfull