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AS-2444697
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAS NO:1287665-60-4
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
AS2444697 是一种口服有效的IRAK-4抑制剂,IC50为 21 nM。它对人和大鼠 IRAK-4 活性具有抑制作用。它通过抗炎作用表现出肾脏保护作用。

产品描述

AS-2444697 is an inhibitor of IRAK-4 (C50 = 21 nM). AS-2444697 exhibits renoprotective effects through anti-inflammatory action. AS-2444697 potently inhibits human and rat IRAK-4 activity.

体外活性

AS-2444697 (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 AS-2444697 (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[1]. After oral administration of AS-2444697 (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[1]. AS-2444697 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[2].

Cas No.

1287665-60-4

储存和溶解度

DMSO:15 mg/mL (34.65 mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years