YM-90709

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的 IL-5 受体拮抗剂，可抑制 IL-5 与其外周人嗜酸性粒细胞和丁酸处理的嗜酸性粒细胞 HL-60 克隆 15 细胞上的受体结合，IC50 分别为 1.0 和 0.57 uM。

A potent IL-5 receptor antagonist that inhibits the binding of IL-5 to its receptor on peripheral human eosinophils and butyric acid-treated eosinophilic HL-60 clone 15 cells with IC50 of 1.0 and 0.57 uM, respectively; inhibits IL-5-prolonged eosinophil survival with IC50 of 0.45 uM and does not affect the GM-CSF-prolonged eosinophil survival; inhibits antigen-induced infiltration of eosinophils and lymphocytes into the bronchoalveolar lavage fluid (BALF) in BN rats (EC50=0.32 mg/kg and 0.12 mg/kg, respectively).

YM-90709 (0-100 μM;1 hour) inhibits the binding of [125I]-IL-5 to IL-5R on human peripheral eosinophils and eosinophilic HL-60 clone 15 cells. YM-90709 (0-100 μM; 96 hour; Eosinophilic HL-60 clone 15 cells) affects IL-5 and GM-CSF and prolonged the survival time of eosinophils. YM-90709 (0-100 μM; 5 min; Eosinophilic HL-60 clone 15 cells) inhibits IL-5-induced, but not GM-CSF-induced, eosinophil survival as well as the tyrosine phosphorylation of Janus kinase 2.Cell Viability Assay Cell Line:Purified eosinophils were suspended at 5×105 cells/ml in RPMI-1640 medium.Concentration:0.01, 0.1, 1, 10 and 100 μM Incubation Time:96 hours Result:The survival time of eosinophils was prolonged.Western Blot Analysis Cell Line:Eosinophilic HL-60 clone 15 cells in RPMI-1640 medium containing 10% FBS, antibiotics, 50 mM 2-ME and 25 mM HEPPES. Concentration:Incubation Time:5 min Result:Reduced the IL-5-induced phosphorylation of JAK2 to near basal levels.

YM-90709 (0.01-10 mg/kg; intravenous injection, 72 hours, Inbred female Brown-Norway (BN) rats) results in the inhibition of antigen-induced infiltration of eosinophils and lymphocytes, but not neutrophils or monocytes, into the bronchoalveolar lavage fluid (BALF) of Brown-Norway (BN) rats. Animal Model:Inbred female Brown-Norway (BN) rats and used at 4-6 weeks of age. Dosage:0.01, 0.1, 1, 10 mg/kg Administration:Intravenous injection; 72 hours Result:Inhibited WBC and eosinophil infiltration in a dose-dependent manner.

YM 90709 | YM90709

Apoptosis

IL Receptor

IL-5

Inflammation/Immunology

——

163769-88-8

359.4211

C22H21N3O2

>98% (HPLC)

10 mM in DMSO

CC(CC1=CC(OC)=C(OC)C=C12)(C)N3C2=CC4=NC5=CC=CC=C5N=C43

Benz[7,8]indolizino[2,3-b]quinoxaline, 5,6-dihydro-2,3-dimethoxy-6,6-dimethyl-

(-20℃)

With Ice Pack

≥ 2 years