AS-2444697 (hydro<wbr/>chloride)

AS-2444697 (hydrochloride)

CAT N°: 29505
Price:

51.00 43.35

AS-2444697 is an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4; IC50 = 21 nM).{52225} It is greater than 30-fold selective for IRAK4 over a panel of 146 kinases, but is less than 10-fold selective over PDGFR?, PDGFR?, TrkA, TrkC, CLK1, Itk, and FLT3. AS-2444697 inhibits IL-1?-induced IL-6 production and LPS-induced TNF-? 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-1?, IL-6, TNF-?, and chemokine (C-C motif) ligand 2 (CCL2) without affecting blood pressure in the 5/6 nephrectomized rat model of chronic kidney disease.{52226}

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