产品描述:
SAR20347 is an inhibitor of the JAK family kinases TYK2 and JAK1-3 (IC50s = 0.6, 23, 26, and 41 nM, respectively, in cell-free assays).{52137} It inhibits IL-12-induced TYK2-dependent phosphorylation of STAT4 in NK-92 cells (IC50 = 126 nM) and IL-6-induced JAK1-dependent STAT3 signaling in TF-1 cells (IC50 = 345 nM). SAR20347 (5 μM) inhibits IL-12-induced INF-γ production and reporter gene activity in peripheral blood mononuclear cells (PBMCs). In vivo, SAR20347 (60 mg/kg) inhibits the production of serum IFN-γ in mice. SAR20347 also reduces keratinocyte activation and skin levels of IL-12, IL-23, IL-6, IL-22, and IFN-γ in a mouse model of psoriasis induced by imiquimod (Item No. 14956).