AS2444697|1287665-60-4|-陌孚医药/Medlife

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AS2444697

目录号: PL04854 纯度: ≥98%

CAS No. :1287665-60-4

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中文名称	AS2444697
中文别名	AS 2444697
英文名称	AS2444697
英文别名	AS 2444697;N-[3-(Aminocarbonyl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl-2-(2-methyl-4-pyridinyl)-4-Oxazolecarboxamide hydrochloride (1:1);N-[3-Carbamoyl-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl]-2-(2-methylpyridin-4-yl)-1,3-oxazole-4-carboxamide;AS2444697, >=98% (HPLC);N-[3-Aminocarbonyl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl]-2-(2-methyl-4-pyridinyl)-4-oxazolecarboxamide hydrochloride;4-Oxazolecarboxamide, N-[3-(aminocarbonyl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl]-2-(2-methyl-4-pyridinyl)-, hydrochloride (1:1);N-[3-carbamoyl-1-(tetrahydro-2h-pyran-4-yl)-1h-pyrazol-4-yl]-2-(2-methylpyridin-4-yl)-1,3-oxazole-4-carboxamide hydrochloride;N-;N-[3-Carbamoyl-1-(oxan-4-yl)pyrazol-4-yl]-2-(2-methylpyridin-4-yl)-1,3-oxazole-4-carboxamide;hydroch;AS2444697
Cas No.	1287665-60-4
分子式	C₁₉H₂₁ClN₆O₄
分子量	432.86
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	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 active IRAK-4 inhibitor with an IC 50 of 21 nM. AS2444697 potently inhibits human and rat IRAK-4 activity. AS2444697 exhibits renoprotective effects through anti-inflammatory action.
性状	Solid
IC50 & Target[1][2]	IRAK4 21 nM (IC50)
体内研究(In Vivo)	AS2444697 is efficacious in the rat adjuvant-induced arthritis (ED 50 2.7 mg/kg, BID, PO) and the rat collagen-induced arthritis (ED 50 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.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. JohnHynesJr, et al. Chapter Nine - Advances in the Discovery of Small-Molecule IRAK4 Inhibitors. Annu Rep Med Chem. 2014 (49):117-133. [2]. Mitsuhiro Kondo, et al. Renoprotective effects of novel interleukin-1 receptor-associated kinase 4 inhibitor AS2444697 through anti-inflammatory action in 5/6 nephrectomized rats. Naunyn Schmiedebergs Arch Pharmacol. 2014 Oct;387(10):909-19.

溶解度数据	In Vitro: DMSO : ≥ 12.5 mg/mL (28.88 mM)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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