生物活性

• 描述YM-90709 is a novel and selective inhibitor against the binding of IL-5 to the IL-5 receptor (IL-5R) with IC50 values of 1.0 and 0.57 μM for blocking the binding of IL-5 to its receptor on peripheral human eosinophils and butyric acid-treated eosinophilic HL-60 clone 15 cells, respectively. YM-90709 inhibited IL-5-induced promotion of the survival of peripheral human eosinophils with IC50 value of 0.45 μM, but did not achieve a complete inhibition of GM-CSF (granulocyte–macrophage colony-stimulating factor)-induced promotion of survival up to 30μM. Similar with that, YM-90709 at 10μM reduced IL-5-induced phosphorylation of JAK2 almost completely, but only reduced GM-CSF-induced phosphorylation to the half level in eosinophilic HL-60 clone 15 cells. These suggested the selectivity of YM-90709 preferentially to blocking the binding of IL-5 to its receptor^[1]. Administration of YM-90709, i.v., inhibited antigen-induced eosinophil and lymphocyte recruitment into the bronchoalveolar lavage fluid (BALF) of Brown-Norway (BN) rats with ED50 values of 0.32 mg/kg and 0.12 mg/kg, respectively, but did not affect the peripheral blood leukocytes or the bone marrow leukocytes, which was contrast to the glucocorticoids^[2].
• 作用机制YM-90709 is an antagonist of IL-5 receptor.^[1]

• 动物研究
  剂量	Rat: 0.01 mg/kg - 10 mg/kg[2] (i.v.)
  给药途径	i.v.