A thiophenecarboxamidopropionate compound that acts as a direct, competitive and high affinity inhibitor of dsRNA binding to TLR3 (Ki=2.96uM; =19nM 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-a and IL-1b (IC90=27uM) and NO production (IC50=3.44uM) in Poly(I:C)-induced RAW 264.7 macrophages. Exhibits minimal cytotoxicity (IC50>100uM in RAW 264.7 cells) and is weakly active against a panel of 12-representative kinases and 4-cytochrome enzymes (in vitro assays).Formula:C18H13ClFNO3SMolecular Weight:377.8Solubility:DMSO (50mg/ml)Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
