产品介绍 Abrocitinib (PF-04965842) 是一种有效的JAK1抑制剂，对JAK1、JAK2、JAK3和TYK2的IC50值分别为29 nM、803 nM、>10000 nM和1250 nM。 Information PF-04965842 is a potentJAK1inhibitor with IC50s of 29 nM, 803 nM, > 10 000 nM and 1250 nM for JAK1, JAK2, JAK3 and tyrosine kinase (TYK) 2, respectively. Targets JAK1 (Cell-free assay); JAK2 (Cell-free assay); TYK2 (Cell-free assay) 29 nM; 803 nM; 1.253 μM In vivo Physicochemical properties and pharmacokinetic parameters of PF-04965842 are examined in rats following doses of 1 mg/kg iv or 3 mg/kg po. Clearance of PF-04965842 is low relative to total liver blood flow (CL = 26.6 mL/min/kg). Vdss = 1.04 L/kg. T 1/2 = 1.1 h. The oral availability of PF-04965842 is 95.6%. PF-04965842 demonstrates efficacy in a dose-responsive manner in a therapeutic rat adjuvant-induced arthritis model.