|
|
| | AS-2444697 Basic information |
| Product Name: | AS-2444697 | | Synonyms: | AS-244469;AS-2444697;N-(3-carbamoyl-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)-2-(2-methylpyridin-4-yl)oxazole-4-carboxamide hydrochloride;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 | | CAS: | 1287665-60-4 | | MF: | C19H21ClN6O4 | | MW: | 432.86084 | | EINECS: | | | Product Categories: | | | Mol File: | 1287665-60-4.mol |  |
| | AS-2444697 Chemical Properties |
| storage temp. | 2-8°C | | solubility | DMSO:16.83(Max Conc. mg/mL);38.88(Max Conc. mM) | | form | powder | | color | white to beige |
| | AS-2444697 Usage And Synthesis |
| 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. | | Uses | 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 | | Biochem/physiol Actions | AS2444697 is a potent and selective inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK-4) that suppresses the progression of chronic renal failure via anti-inflammatory action. | | storage | Desiccate at RT |
| | AS-2444697 Preparation Products And Raw materials |
|