YM-90709
产品说明书
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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 |
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| 溶解度 : | - | |
| 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 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.78mL 0.56mL 0.28mL |
13.91mL 2.78mL 1.39mL |
27.82mL 5.56mL 2.78mL |
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