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YM-90709
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
YM-90709图片
CAS NO:163769-88-8
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 359.42
Formula C22H21N3O2
CAS No. 163769-88-8
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 10 mM
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo) CC(CC1=CC(OC)=C(OC)C=C12)(C)N3C2=CC4=NC5=CC=CC=C5N=C43
Synonyms YM-90709; YM 90709; YM90709.
实验参考方法
In Vitro

In vitro activity: YM-90709 is a novel antagonist of interleukin-5 receptor which inhibits the binding of interleukin-5 to interleukin-5 receptor. YM-90709 inhibit the binding of IL-5 to its receptor on peripheral human eosinophils and butyric acid-treated eosinophilic HL-60 clone 15 cells, with IC50 values of 1.0 and 0.57 microM, respectively. Interleukin-5 (IL-5) plays an important role in the activation of eosinophils in allergic inflammation including asthma and atopic dermatitis. In contrast, YM-90709 did not affect the binding of granulocyte-macrophage colony-stimulating factor (GM-CSF) to its receptor on eosinophils and eosinophilic HL-60 clone 15 cells. In functional assays, YM-90709 inhibited IL-5-prolonged eosinophil survival with an IC50 value of 0.45 microM and did not affect the GM-CSF-prolonged eosinophil survival. Furthermore, YM-90709 inhibited the IL-5-induced but not GM-CSF-induced tyrosine phosphorylation of Janus kinase 2 (JAK2) in eosinophilic HL-60 clone 15 cells. These results indicate that YM-90709 is a novel IL-5 inhibitor which selectively blocks the binding of IL-5 to the IL-5 receptor (IL-5R).


Kinase Assay: YM-90709 is a novel antagonist of interleukin-5 receptor which inhibits the binding of interleukin-5 to interleukin-5 receptor. YM-90709 inhibit the binding of IL-5 to its receptor on peripheral human eosinophils and butyric acid-treated eosinophilic HL-60 clone 15 cells, with IC50 values of 1.0 and 0.57 microM, respectively.


Cell Assay: YM-90709 inhibited the IL-5-induced but not GM-CSF-induced tyrosine phosphorylation of Janus kinase 2 (JAK2) in eosinophilic HL-60 clone 15 cells. These results indicate that YM-90709 is a novel IL-5 inhibitor which selectively blocks the binding of IL-5 to the IL-5 receptor (IL-5R).

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.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
Animal model Rats with antigen-induced airway inflammation
Formulation & Dosage
References Int Immunopharmacol. 2002 Nov;2(12):1693-702.Immunol Lett. 2005 Apr 15;98(1):161-5.Int Immunopharmacol. 2004 Jul;4(7):873-83.