AS 2444697

SKU: orb1941100

Description

A potent, selective, orally bioavailable IRAK-4 inhibitor that potently inhibits human and rat IRAK-4 activity with subnanomolar order, >30-fold selectivity over IRAK-1; inhibited IL-1β- or TLR ligand lipopolysaccharide (LPS)-induced IL-6 production in human lung alveolar epithelial cells, fibroblast-like synoviocytes, and peripheral blood mononuclear cells; significantly reduces urinary protein excretion and preventd the development of glomerulosclerosis and interstitial fibrosis without affecting the blood pressure in mice model of chronic kidney disease.

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Key Properties

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CAS Number	1287665-60-4
MW	432.865
Purity	>98% (HPLC)
Formula	C₁₉H₂₁ClN₆O₄
SMILES	CC1=NC=CC(=C1)C2=NC(=CO2)C(=O)NC3=CN(N=C3C(=O)N)C4CCOCC4.Cl
Target	IRAK
Solubility	In Vitro: DMSO : ≥ 12.5 mg/mL (28.88 mM)

Bioactivity

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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. 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. Animal model: Male 6-week-old Wistar rats and Balb/c mice. 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.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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AS2444697 | AS-2444697

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IRAK

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AS 2444697 (orb1941100)

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Purity:	97.43% (May vary between batches)
CAS Number:	1287665-60-4
MW:	432.86
Formula:	C₁₉H₂₁ClN₆O₄

AS 2444697

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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AS 2444697 (orb1941100)

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