Baricitinib phosphate

  • Chemical Properties
CAS No. 1187595-84-1 Cat. No. BCP15527
Name Baricitinib phosphate
Synonyms INCB-28050;INCB28050;INCB 28050;LY3009104;LY 3009104;LY-3009104;
Formula C16H20N7O6PS M. Wt 469.41
  • Biological Activity
Description INCB028050 inhibits intracellular signaling of multiple proinflammatory cytokines including IL-6 and IL-23 at concentrations <50 nM. Significant efficacy, as assessed by improvements in clinical, histologic and radiographic signs of disease, was achieved in the rat adjuvant arthritis model with doses of INCB028050 providing partial and/or periodic inhibition of JAK1/JAK2 and no inhibition of JAK3 . in vivo: The efficacy following daily oral administration of INCB028050 was assessed at doses of 1, 3, or 10 mg/kg based on its pharmacokinetic profile in this species. Disease severity was assessed periodically, scoring clinical signs of disease. These doses were based on the PK/PD relationship established with the IL-6 WBA, with the goal of inhibiting JAK1/2 signaling by no more than 50% for half of the day. Relative to vehicle-treated animals, increasing doses of INCB028050 inhibited disease scores by 24% (p < 0.05), 57% (p < 0.01), and 81% (p < 0.01), respectively . Baricitinib preferent
Pathways Angiogenesis/Protein Tyrosine Kinase Jak/Stat Pathway Wnt/Stem Cell Epigenetics 
Targets JAK 

Structure

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