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Beschreibung

A thiophenecarboxamidopropionate compound that acts as a direct, competitive and high affinity inhibitor of dsRNA binding to TLR3 (Ki = 2.96 microM, Kd = 19 nM for dsRNA binding to TLR3) and selectively antagonizes stimulated TLR3 signaling without affecting TLR1/2, TLR2/6, TLR4 and TLR7 pathways. Shown to efficiently repress TNF-&alpha, and IL-1&beta, (IC90 = 27 microM) and NO production (IC50 = 3.44 microM) in Poly(I:C)-induced RAW 264.7 macrophages. Exhibits minimal cytotoxicity (IC50 >>100 microM in RAW 264.7 cells) and is weakly active against a panel of 12-representative kinases and 4-cytochrome enzymes (in vitro assays).