Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 378 | 现货 | ||
5 mg | ¥ 913 | 现货 | ||
10 mg | ¥ 1,390 | 现货 | ||
25 mg | ¥ 2,820 | 现货 | ||
50 mg | ¥ 4,570 | 现货 | ||
100 mg | ¥ 7,890 | 现货 | ||
200 mg | ¥ 10,600 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,060 | 现货 |
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. |
靶点活性 | IRAK4:21 nM |
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]. |
分子量 | 432.86 |
分子式 | C19H21ClN6O4 |
CAS No. | 1287665-60-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 15 mg/mL (34.65 mM), Sonication and heating to 60℃ are recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3102 mL | 11.5511 mL | 23.1022 mL | 57.7554 mL |
5 mM | 0.462 mL | 2.3102 mL | 4.6204 mL | 11.5511 mL | |
10 mM | 0.231 mL | 1.1551 mL | 2.3102 mL | 5.7755 mL | |
20 mM | 0.1155 mL | 0.5776 mL | 1.1551 mL | 2.8878 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
AS-2444697 1287665-60-4 Immunology/Inflammation NF-Κb IRAK IL-1R associated kinase AS2444697 IRAK-4 anti-inflammatory AS 2444697 inhibit renoprotective Inhibitor Interleukin-1 receptor associated kinase inhibitor