AS2444697_product_DataBase

Bioactivity	AS2444697 is an orally active IRAK-4 inhibitor with an IC50 of 21 nM[1]. AS2444697 potently inhibits human and rat IRAK-4 activity. AS2444697 exhibits renoprotective effects through anti-inflammatory action[2].
In Vivo	AS2444697 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[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:
Name	AS2444697
CAS	1287665-60-4
Formula	C19H21ClN6O4
Molar Mass	432.86
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[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.

PeptideDB

AS2444697

CAS: 1287665-60-4 F: C19H21ClN6O4 W: 432.86