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[CAS NO. 1287665-60-4] AS2444697
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-18992 |
| Brand: | MCE |
| CAS: | 1287665-60-4 |
Overview
| MDL | MFCD30182294 |
|---|---|
| Molecular Weight | 432.86 |
| Molecular Formula | C19H21ClN6O4 |
| SMILES | O=C(NC1=CN(C2CCOCC2)N=C1C(N)=O)C3=COC(C4=CC=NC(C)=C4)=N3.[H]Cl |
Summary
IC50 & Target
|
IRAK4 21 nM (IC 50 ) |
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
[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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Appearance
Solid
Shipping
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)
Solvent & Solubility
DMSO : ≥ 12.5 mg/mL ( 28.88 mM )
* "≥" means soluble, but saturation unknown.
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 |
References
- [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.
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