AS-2444697
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AS-2444697
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CAS No:
1287665-60-4
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Formula:
C19H21ClN6O4
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Chemical Name:
AS-2444697
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Synonyms:
AS-2444697;N-(3-carbamoyl-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)-2-(2-methylpyridin-4-yl)oxazole-4-carboxamide hydrochloride;AS-244469;N-(3-CARBAMOYL-1-(TETRAHYDRO-2H-PYRAN-4-YL)-1H-PYRAZOL-4-YL)-2-(2-METHYLPYRIDIN-4-YL)OXAZOLE-4-CARBOXAMIDE HCL;4-Oxazolecarboxamide, N-[3-(aminocarbonyl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl]-2-(2-methyl-4-pyridinyl)-, hydrochloride (1:1);AS-2444697 HCl;FGNHLIIFEDYNFZ-UHFFFAOYSA-N;N-[3-Aminocarbonyl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl]-2-(2-methyl-4-pyridinyl)-4-oxazolecarboxamide hydrochloride
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CAS No:
Description
AS-2444697 is an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4; IC50= 21 nM). It is greater than 30-fold selective for IRAK4 over a panel of 146 kinases, but is less than 10-fold selective over PDGFRα, PDGFRβ, TrkA, TrkC, CLK1, Itk, and FLT3. AS-2444697 inhibits IL-1β-induced IL-6 production and LPS-induced TNF-α production in cellular assays (IC50s = 250 and 47 nM, respectively). It is efficacious in rat models of adjuvant- and collagen-induced arthritis (ED50s = 2.7 and 1.6 mg/kg, respectively). AS-2444697 (0.3-3 mg/kg, twice daily) reduces urinary protein excretion, the development of interstitial fibrosis and glomerulosclerosis, and renal mRNA expression of genes encoding IL-1β, IL-6, TNF-α, and chemokine (C-C motif) ligand 2 (CCL2) without affecting blood pressure in the 5/6 nephrectomized rat model of chronic kidney disease.
AS-2444697 Use and Manufacturing
AS2444697 has been used as an interleukin-1R-associated kinase 4 (IRAK4) inhibitor to study the role of interleukin (IL)-1/IL-33 signaling in the development of endometriosis using a mouse model of endometriosis. It has also been used to study its dose-dependent effect on the C-X-C motif chemokine ligand 8 (CXCL8) gene expression
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