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Nemiralisib

CAS No. : 1254036-71-9

MCE 国际站：Nemiralisib

产品活性：Nemiralisib (GSK2269557 free base) 是一种有效的选择性 PI3Kδ 抑制剂，pK_i 为 9.9。

研究领域：PI3K/Akt/mTOR

作用靶点：PI3K

In Vitro: Nemiralisib (GSK2269557 free base) is highly selective for PI3Kδ, with >1000-fold selectivity over the closely related isoforms PI3Kα (pIC₅₀=5.3), PI3Kβ (pIC₅₀=5.8) and PI3Kγ (pIC₅₀=5.2). Nemiralisib inhibits IFNγ in the peripheral blood mononuclear (PBMC) assay with an pIC₅₀ of 9.7.

In Vivo: To assess the suitability of the series for inhaled delivery clearance data in rat microsomes and subsequently in vivo pharmacokinetic data from Sprague Dawley male rats is obtained. Compounds (e.g., Nemiralisib) are administered by the oral or intravenous routes, at a dose level of 3 and 1mg/kg respectively (n=2 rats/route). Nemiralisib free base is active in a disease relevant brown norway rat acute OVA model of Type 2 helper T-cells (Th2)-driven lung inflammation.

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