TAK-242TAK-242 (Resatorvid), a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, inhibits the production of lipopolysaccharide-induced inflammatory mediators by binding to the intracellular domain of TLR4.
IC50 value: 1.1-11 nM [1]
Target: TLR4
in vitro: In RAW264.7 cells and mouse peritoneal macrophages, TAK-242 suppressed lipopolysaccharide (LPS)-induced production of NO, tumor necrosis factor-alpha (TNF-alpha), and interleukin (IL)-6, with 50% inhibitory concentration (IC50) of 1.1 to 11 nM.
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Description: Orteronel (TAK-700 R-form) is a naphthylmethylimidazole derivative.Orteronel (TAK-700 R-form) is a highly selective 17,20-lyase inhibitor with potential utility in the treatment of prostate cancer.