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苏州工业园区生物纳米园A4#216
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4000-520-616 / 18915418616
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0512-67156496
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商品描述
| Description | Upadacitinib(ABT-494)isaselectiveJAK1inhibitorwhichdemonstratesactivityagainstJAK1(0.045μM)andJAK2(0.109μM),with>40foldselectivityoverJAK3(2.1μM)and100foldselectivityoverTYK2(4.7μM)ascomparedtoJAK1. | ||||
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| Targets |
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| Invitro | UpadacitinibismostpotentonJAK1comparedtootherfamilymembers(JAK1 > JAK2 > JAK3 > TYK2).Upadacitinibdemonstratesselectivityacrossabroadpanelof70+kinases,withonlyRock1andRock2demonstratingIC50valuesbelow1μM.ConsistentwiththeBa/F3cellulardata,upadacitinibpotentlyinhibitstheJAK1dependentcytokinesIL-6,OSM,IL-2,andIFNγ,asmeasuredbyinhibitionofSTATphosphorylation[1]. | ||||
| Invivo | Upadacitinibinhibitsdiseasepathologyinratadjuvantinducedarthritis[1].Itisanon-sensitivesubstrateforcytochromeP450,approximately20%iseliminated,unchanged,inurine[2]. |
