货号:A805441 同义名: AS-2444697 (hydrochloride)
AS 2444697 is a potent and selective interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with IC50 of 21 nM.
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描述 | AS2444697, an orally active IRAK-4 inhibitor, shows an IC50 of 21 nM, effectively inhibiting both human and rat IRAK-4 activity[1]. AS2444697 also exerts renoprotective effects through its anti-inflammatory actions[2]. |
体内研究 | Demonstrating efficacy in rat adjuvant-induced arthritis (with an ED50 of 2.7 mg/kg, administered twice daily orally) and rat collagen-induced arthritis (ED50 of 1.6 mg/kg, BID, PO) disease models, AS2444697 reveals good bioavailability in pharmacokinetic studies conducted on rats (F% 50) and dogs (F% 78)[1]. In LPS/GalN-treated mice, AS2444697, administered at doses ranging from 0.3 to 3 mg/kg, significantly elevates plasma levels of IL-1β, IL-6, TNF-α, MCP-1, and aminotransferases (ALT and AST). A single administration of AS2444697 dose-dependently reduces the plasma levels of these parameters, with significant effects observed at doses of 1 mg/kg or higher[2]. Following oral administration to 5/6 nephrectomized (Nx) rats at a dose of 3 mg/kg, the peak plasma and tissue (liver and kidney) concentrations of AS2444697 are observed at 1 hour, gradually decreasing thereafter, with a terminal half-life of approximately 2.7-2.9 hours[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.31mL 0.46mL 0.23mL |
11.55mL 2.31mL 1.16mL |
23.10mL 4.62mL 2.31mL |
CAS号 | 1287665-60-4 |
分子式 | C19H21ClN6O4 |
分子量 | 432.861 |
别名 | AS-2444697 (hydrochloride) |
运输 | 蓝冰 |
存储条件 |
粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 12 mg/mL(27.72 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |