YM-90709

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Chemical Structure| 163769-88-8 同义名 : -
CAS号 : 163769-88-8
货号 : A265624
分子式 : C22H21N3O2
纯度 : 99%+
分子量 : 359.42
MDL号 : MFCD00354370
存储条件：

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(166.94 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.78mL

0.56mL

0.28mL

13.91mL

2.78mL

1.39mL

27.82mL

5.56mL

2.78mL
参考文献

[1]Morokata T, Ida K, et al. Characterization of YM-90709 as a novel antagonist which inhibits the binding of interleukin-5 to interleukin-5 receptor. Int Immunopharmacol. 2002 Nov;2(12):1693-702.

[2]Morokata T, Suzuki K, et al. 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. Int Immunopharmacol. 2004 Jul;4(7):873-83.