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

Boiling point:

579.6±50.0 °C(Predicted)

Density 

1.28±0.1 g/cm3(Predicted)

storage temp. 

Sealed in dry,Room Temperature

solubility 

DMF: 10 mg/ml; DMSO: 20 mg/ml; Ethanol: 2 mg/ml

form 

A crystalline solid

pka

2.74±0.40(Predicted)

color 

Brown to orange

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

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.

in vivo

IC 50

IL-5

References

[1] TATSUAKI MOROKATA  Toshimitsu Y  Kenji Ida. Characterization of YM-90709 as a novel antagonist which inhibits the binding of interleukin-5 to interleukin-5 receptor[J]. International immunopharmacology, 2002, 2 12: Pages 1693-1702. DOI: 10.1016/s1567-5769(02)00191-1
[2] TATSUAKI MOROKATA. Effect of a novel interleukin-5 receptor antagonist, YM-90709 (2,3-dimethoxy-6,6-dimethyl-5,6-dihydrobenzo[7,8]indolizino[2,3-b]quinoxaline), on antigen-induced airway inflammation in BN rats[J]. International immunopharmacology, 2004, 4 7: Pages 873-883. DOI: 10.1016/j.intimp.2004.03.011
[3] TATSUAKI MOROKATA. Effect of a novel interleukin-5 receptor antagonist, YM-90709, on antigen-induced eosinophil infiltration into the airway of BDF1 mice[J]. Immunology letters, 2005, 98 1: Pages 161-165. DOI: 10.1016/j.imlet.2004.11.003

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