AS2444697,1287665-60-4

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AS2444697

CAS No. : 1287665-60-4

MCE 国际站：AS2444697

产品活性：AS2444697 是一种具有口服活性的 IRAK-4 抑制剂，IC₅₀ 为 21 nM。 AS2444697 有效抑制人和大鼠 IRAK-4 活性。AS2444697 通过抗炎作用表现出肾脏保护作用。

研究领域：Immunology/Inflammation

作用靶点：IRAK

In Vivo: AS2444697 is efficacious in the rat adjuvant-induced arthritis (ED₅₀ 2.7 mg/kg, BID, PO) and the rat collagen-induced arthritis (ED₅₀ 1.6 mg/kg, BID, PO) disease models. Good bioavailability was seen in rat (F% 50) and dog (F% 78) pharmacokinetic studies.
AS2444697 (0.3-3 mg/kg) significantly increases the plasma levels of IL-1β, IL-6, TNF-α, MCP-1, and aminotransferases (ALT and AST) in LPS/GalN-treated mice. Single administration of AS2444697 (0.3-3 mg/kg) dose-dependently decreases plasma levels of these all parameters, and these effects were significant at doses of 1 mg/kg or higher.
After oral administration of AS2444697 (3 mg/kg) to 5/6 Nx rats, plasma, and tissue (liver and kidney) concentrations of the unchanged drug peaked at 1 h and then gradually decreased, with a terminal half-life of 2.7-2.9 h.

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