5,6-DIHYDRO-2,3-DIMETHOXY-6,6-DIMETHYLBENZ[7,8]INDOLIZINO[2,3-B]QUINOXALINE

Description

YM-90709 is a competitive antagonist of the interleukin-5 (IL-5) receptor that has IC₅₀ values of 1 and 0.57 μM for peripheral human eosinophils and eosinophilic HL-60 clone 15 cells, respectively, in a radioligand binding assay. It inhibits IL-5-induced eosinophil survival (IC₅₀ = 0.45 μM) and JAK2 phosphorylation in vitro. YM-90709 inhibits eosinophil and lymphocyte infiltration (ED₅₀s = 0.32 and 0.12 mg/kg, respectively) into the brochoalveolar lavage fluid (BALF) of rats and eosinophil infiltration (ED₅₀ = 0.05 mg/kg) into the BALF of mice in models of airway inflammation.

Uses

YM 90709, is an interleukin-5 receptor antagonist.

Definition

ChEBI: LSM-2128 is a quinoxaline derivative.

Biological Activity

Novel, selective inhibitor of interleukin-5 (IL-5) binding to its receptor (IC 50 = 0.45-1 mM). Inhibits IL-5-prolonged eosinophil survival and IL-5-induced tyrosine phosphorylation of JAK2 without inhibiting GM-CSF-mediated effects. In vivo, inhibits antigen-induced eosinophil and lymphocyte recruitment in rat airways, without affecting peripheral blood or bone marrow leukocytes.