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。
| 生物活性 | AS2444697 is an orally activeIRAK-4inhibitor with anIC50of 21 nM[1]. AS2444697 potently inhibits human and rat IRAK-4 activity. AS2444697 exhibits renoprotective effects through anti-inflammatory action[2]. |
| IC50& Target | |
体内研究
(In Vivo) | AS2444697 is efficacious in the rat adjuvant-induced arthritis (ED502.7 mg/kg, BID, PO) and the rat collagen-induced arthritis (ED501.6 mg/kg, BID, PO) disease models. Good bioavailability was seen in rat (F% 50) and dog (F% 78) pharmacokinetic studies[1].
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[2].
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[2].
| Animal Model: | Male 6-week-old Wistar rats and Balb/c mice[2] | | Dosage: | 0.3-3 mg/kg | | Administration: | Single administration; orally | | Result: | The plasma levels of IL-1β, IL-6, TNF-α, MCP-1, and aminotransferases (ALT and AST) were significantly increased. |
|
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : ≥ 12.5 mg/mL(28.88 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.3102 mL | 11.5511 mL | 23.1022 mL | | 5 mM | 0.4620 mL | 2.3102 mL | 4.6204 mL | | 10 mM | 0.2310 mL | 1.1551 mL | 2.3102 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 1.67 mg/mL (3.86 mM); Suspended solution; Need ultrasonic
此方案可获得 1.67 mg/mL (3.86 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 1.67 mg/mL (3.86 mM); Clear solution
此方案可获得 ≥ 1.67 mg/mL (3.86 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
m.cnreagent.com