1. IRAK
  2. AS2444697

AS2444697 

Cat. No.: HY-18992
Handling Instructions

AS2444697 is an orally active IRAK-4 inhibitor with an IC50 of 21 nM. AS2444697 potently inhibits human and rat IRAK-4 activity. AS2444697 exhibits renoprotective effects through anti-inflammatory action.

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AS2444697 Chemical Structure

AS2444697 Chemical Structure

CAS No. : 1287665-60-4

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Description

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].

IC50 & Target[1]

IRAK4

21 nM (IC50)

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: 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.
Molecular Weight

432.86

Formula

C₁₉H₂₁ClN₆O₄

CAS No.

1287665-60-4

SMILES

O=C(NC1=CN(C2CCOCC2)N=C1C(N)=O)C3=COC(C4=CC=NC(C)=C4)=N3.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : ≥ 25 mg/mL (57.76 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

AS2444697AS 2444697AS-2444697IRAKInterleukin-1 receptor associated kinaseIL-1R associated kinaseIRAK-4renoprotectiveanti-inflammatoryInhibitorinhibitorinhibit

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AS2444697
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