Cas No.: | 163769-88-8 |
Chemical Name: | YM 90709,YM90709,YM-90709 |
Synonyms: | YM 90709,YM90709,YM-90709 |
SMILES: | CC1(CC2=CC(=C(C=C2C3=CC4=NC5=CC=CC=C5N=C4N31)OC)OC)C |
Formula: | C22H21N3O2 |
M.Wt: | 359.42 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | YM-90709 is a novel antagonist which inhibits the binding of interleukin-5 to interleukin-5 receptor. |
In Vivo: | YM-90709 suppresses antigen-induced airway inflammation in Brown Norway rats . YM-90709 is a novel IL-5R antagonist with those of anit-IL-5 mAb on the antigen-induced infiltration of eosinophils into the airways of BDF1 mice, a strain that is commonly used in the antibody estimation. [2] This is the first report on the examination of the effects of YM-90709 in vivo, as a novel IL-5R antagonist on the antigen-induced infiltration of eosinophils and other leukocytes into the BALF of Brown-Norway (BN) rats. [3] |
In Vitro: | YM-90709 potently inhibits the binding of 100 pM [125I]-IL-5 to IL-5R on human peripheral eosinophils and eosinophilic HL-60 clone 15 cells with IC50 values of 1.0±0.40 and 0.57±0.21 μM, respectively. YM-90709 inhibits the 4 pM IL-5-induced effect in a concentration-dependent manner with an IC50 value of 0.45±0.024 μM. YM-90709 also inhibits the higher concentrations (12 and 40 pM) of IL-5-induced effects with IC50 values of 0.89±029 and 1.0±0.22 μM, respectively. [1] YM-90709 is a novel interleukin-5 receptor antagonist, YM-90709 inhibits antigen-induced eosinophil recruitment into the airway, the same as anti-IL-5 mAb does. YM-90709 inhibits the binding of IL-5 to IL-5R on human eosinophils, but did not inhibit the binding of GM-CSF to GM-CSFR. In addition, YM-90709 inhibits IL-5-induced, but not GM-CSF-induced, eosinophil survival as well as the tyrosine phosphorylation of Janus kinase 2. [2] |