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。 Resatorvid 抑制自噬 (autophagy)，并在各种炎症性疾病中起关键作用。 * Please select Quantity before adding items. • Signal Transduct Target Ther. 2024 Mar 25;9 (1):74. [Abstract] • Nature. 2023 Jun;618 (7964):374-382.

2020年1月20日 · In this study, we postulated that the pharmacological inhibition of TLR4 by TAK-242 may alleviate LPS-induced muscle wasting by suppressing activation of inflammatory and proteolytic pathways,...

TAK-242 completely prevented LPS-induced inflammation and insulin resistance in muscle cells. Reduced signalling through the NF-κB and MAPK pathways followed by restored insulin-stimulated Akt phosphorylation provide a mechanism for the ability of TAK-242 to protect against LPS-induced insulin resistance.

A novel cyclohexene derivative, ethyl (6R)-6-[N-(2-Chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate (TAK-242), selectively inhibits toll-like receptor 4-mediated cytokine production through suppression of intracellular signaling.

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.

2007年10月1日 · TAK-242 has been shown to inhibit LPS-induced intracellular signaling without inhibiting LPS binding to cells and strongly suppress TLR4-mediated cytokine and nitric oxide (NO) production from monocytes and macrophages (Ii et al., 2006).

1 天前 · In human monocytes, TAK-242 significantly decreased LPS-induced TNF-α and IL-6 secretion while preserving anti-inflammatory cytokines such as IL-10. This selective suppression suggests TAK-242 does not entirely shut down immune signaling but shifts the balance toward a less inflammatory state. In rodent models of endotoxemia, TAK-242 ...

2020年1月20日 · Notably, pretreatment of cells or mice with TAK-242 reduced or reversed all the detrimental effects of LPS in vitro and in vivo. Collectively, our results indicate that pharmacological inhibition of TLR4 signalling may be a novel therapeutic intervention for endotoxemia-induced muscle wasting.

Resatorvid (TAK-242, CLI-095, TAK242, CLI095)，又称瑞沙托维，是TLR4信号的选择性抑制剂，具有抗炎活性。 Resatorvid通过与TLR4胞内区域的Cys747残基直接结合，破坏TLR4与衔接子分子TIRAP和TRAM的相互作用，进而抑制TLR4信号。

2007年10月1日 · These results suggest that TAK-242 protects mice against LPS-induced lethality by inhibiting production of multiple cytokines and NO. TAK-242 has a quick onset of action and provides significant benefits by post-treatment, suggesting that it may be a promising drug candidate for the treatment of sepsis.