Resatorvid (TAK-242) 是一种选择性的 TLR4 信号传导抑制剂。 Resatorvid 抑制 NO，TNF-α 和 IL-6 的产生，其 IC50 值分别为 1.8 nM，1.9 nM，1.3 nM。 Resatorvid 下调 TLR4 下游信号分子 MyD88 和 TRIF 的表达。

2008年4月14日 · TAK-242, a small-molecule antisepsis agent, has shown to suppress lipopolysaccharide (LPS)-induced inflammation. In this study, we demonstrate that TAK-242 is a selective inhibitor of Toll-like receptor (TLR)-4 signaling.

2020年1月20日 · Using C2C12 myotubes in vitro and a mouse model of endotoxemia in vivo, we found that TAK-242, a selective inhibitor of TLR4-mediated signalling, blocked systemic and skeletal muscle...

TAK-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. Cys747 in TLR4 has been identified previously as …

TAK-242 (resatorvid) is a small-molecule compound that selectively inhibits TLR4 signaling. TAK-242 inhibits the TLR4 pathway by binding directly to a Cys747 in the intracellular TLR4 domain . It has been observed that TAK-242 disrupts the interactions of TLR4 with its adaptor molecules, TIRAP (toll-interleukin 1 receptor (TIR) domain ...

TAK-242 (resatorvid), a cyclohexene derivative, is a small-molecule inhibitor of TLR4 signalling, which was originally characterized as a novel anti-sepsis agent capable of inhibiting inflammatory mediator production .

生物活性：Resatorvid (TAK-242) 是一种选择性 Toll 样受体 4 (TLR4) 抑制剂。 Resatorvid 抑制 NO、TNF-α 和 IL-6 的产生，IC50s 分别为 1.8 nM、1.9 nM 和分别为 1.3 nM。 Resatorvid 下调 TLR4 下游信号分子 MyD88 和 TRIF 的表达。

2010年8月9日 · TAK-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. Cys747 in TLR4 has been identified previously as the binding site of TAK-242.

TAK-242 inhibited the expression of TLR4/NF-κB/NLRP3 signalling related-proteins, decreased the levels of 24 h urinary protein, serum creatinine, circular immune complex (CIC) and kidney immunoglobulin A (IgA), and improved renal histopathological damage in HH-HSPN rats.

Inhibition of Toll-like receptor 4 (TLR4)-mediated inflammatory pathways exerts a critical effect on neuronal death; therefore, it is a possible new therapeutic approach for traumatic brain injury (TBI). Resatorvid (TAK-242) is a novel ...