General description
一种抑制IL-5与IL-5受体结合的抑制剂。
YM-90709 is a novel antagonist which inhibits the binding of interleukin-5 to interleukin-5 receptor. Target: IL-5 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. 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. 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.
YM-90709是一种新型拮抗剂，可抑制白介素5与白介素5受体的结合。靶标：体外IL-5：YM-90709有效抑制100 pM [125I] -IL-5与人外周血嗜酸性粒细胞和嗜酸性HL-60克隆15细胞上IL-5R的结合，IC50值为1.0±0.40和0.57分别为±0.21μM。 YM-90709以浓度依赖的方式抑制4 pM IL-5诱导的作用，IC50值为0.45±0.024μM。 YM-90709还抑制更高浓度的IL-5诱导的作用（12和40 pM），IC50值分别为0.89±029和1.0±0.22μM。 YM-90709是新型的白介素5受体拮抗剂，与抗IL-5 mAb一样，YM-90709抑制抗原诱导的嗜酸性粒细胞募集进入气道。 YM-90709抑制人嗜酸性粒细胞上IL-5与IL-5R的结合，但不抑制GM-CSF与GM-CSFR的结合。此外，YM-90709抑制IL-5诱导，但不抑制GM-CSF诱导的嗜酸性粒细胞存活以及Janus激酶2的酪氨酸磷酸化。体内：YM-90709抑制褐挪威大鼠中抗原诱导的气道炎症。 YM-90709是一种新颖的IL-5R拮抗剂，与anit-IL-5 mAb的拮抗剂对抗原诱导的嗜酸性粒细胞向BDF1小鼠气道的浸润有关，BDF1小鼠是一种通常用于抗体评估的菌株。这是关于YM-90709作为一种新的IL-5R拮抗剂在体内对抗原诱导的嗜酸性粒细胞和其他白细胞浸入Brown-Norway（BN）大鼠BALF的作用的研究的第一份报告。
Properties
| Iupac Name： | 2,3-dimethoxy-6,6-dimethyl-5,6-dihydrobenzo[7,8]indolizino[2,3-b]quinoxaline |
| Inchi Code | 1S/C22H21N3O2/c1-22(2)12-13-9-19(26-3)20(27-4)10-14(13)18-11-17-21(25(18)22)24-16-8-6-5-7-15(16)23-17/h5-11H,12H2,1-4H3 |
| Inchi Key | HIXSPVQXXDULHS-UHFFFAOYSA-N |
安全信息
RIDADR NONH for all modes of transport
