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Enpatoran

產(chǎn)品活性：Enpatoran (M5049) 是一種有效的、具有口服活性的 TLR7/8 抑制劑，在HEK293 細(xì)胞中，其IC₅₀s 分別為 11.1 nM 和 24.1 nM。Enpatoran 對 TLR3, TLR4 和 TLR9 無活性。Enpatoran 可以阻斷分子合成配體和天然內(nèi)源性 RNA 配體。Enpatoran 在體內(nèi)的表現(xiàn)出良好的藥代動力學(xué)特性。Enpatoran 可用于先天性和適應(yīng)性自身免疫阻斷的相關(guān)研究。

研究領(lǐng)域：Immunology/Inflammation

作用靶點：Toll-like Receptor (TLR)

In Vitro: Enpatoran (0.01 nM-10 μM) inhibits production of IL-6 stimulated by all the ligands (miR-122, Let7c RNA, Alu RNA, and R848) with IC₅₀ values ranging from 35 to 45 nM.

In Vivo: Pre-treatment with Enpatoran (M5049; oral gavage; 1 mg/kg) before R848 (intraperitoneal injection of 25 µg) dose-dependently inhibits the production of IL-6 and IFN-α in mice.
Enpatoran (M5049) exhibits high oral bioavailability (mouse 100%, rat 87%, dog 84%) following oral administration (mouse, rat and dog 1.0 mg/kg).
Enpatoran exhibits moderate half-lives (mouse 1.4, rat 5.0 and dog 13 h) due to high plasma clearance (1.4, 1.2 and 0.59 L/h/kg, respectively) combined with large volumes of distribution (2.7, 8.7 and 5.7 L/kg, respectively) following intravenous administration (mouse, rat and dog 1.0 mg/kg).

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