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GSK2245035

CAS No. : 1207629-49-9

MCE 国际站：GSK2245035

产品活性：GSK2245035 是一种高效的，选择性的鼻内 Toll-Like 受体 7 (TLR7) 激动剂，具有优先刺激 1 型干扰素 (IFN) 的特性。GSK2245035 对 IFNα 和TNFα 的 pEC₅₀ 分别为 9.3 和 6.5。GSK2245035 有效抑制人外周血细胞培养物中过敏原诱导的 Th2 细胞因子产生。GSK2245035 有用于哮喘的潜力。

研究领域：Immunology/Inflammation  |  Apoptosis

作用靶点：Toll-like Receptor (TLR)  |  IFNAR  |  TNF Receptor

In Vitro: GSK2245035 (0.01, 0.1, 1, 10, 100, 1000, 10000 nM; 6 days) reduces levels of the Th2 cytokines IL-5 and IL-13 released in response to Timothy grass or house dust mite in human PBMC cultures derived from individuals allergic to these allergens, in a dose-dependent manner.

In Vivo: GSK2245035 (i.n.; 0.03-1 mg/kg; 6 hours) makes dose-related increasing in IFNα levels in serum at doses of 0.3 mg/kg and above at the 2 h time point which had subsided at 6 h.
GSK2245035 (3, 30, 300, 3000 ng/kg; 6 hours) treatment can make plasma IP-10 provided the most sensitive biomarker of target engagement with raised levels of this chemokine detected at doses of 30 ng/kg and above in the cynomolgus monkey.

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