| 货号 | 13871-25mg |
| 描述 | Toll-like receptor 4 (TLR4) is activated by lipopolysaccharide (LPS), with LPS-binding protein, to initiate an innate immune response.1 Alternatively, hypoxia or ischemia/reperfusion can trigger signaling through TLR4.2 TAK-242 is a cell-permeable inhibitor of TLR4 signaling, blocking LPS-induced production of NO, TNF-α, IL-6, and IL-1β in macrophages with IC50 values of 1-11 nM.3,4 It does not affect signaling through other TLRs.3,4,5 TAK-242 is effective in vivo, suppressing the production of NO, TNF-α, IL-6, and IL-1β in mice treated with LPS when given intravenously.3 Mechanistically, TAK-242 acts by selectively binding TLR4 and preventing its association with adaptor proteins that are essential for signal transduction.5 TAK-242 is used to study signaling through TLR4 in a variety of pathologies, including sepsis and ischemia/reperfusion injury.6,7 |
| 别名 | Resatorvid; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Morris, M.C.,Gilliam, E.A. and Li, L. Innate immune programing by endotoxin and its pathological consequences. Front.Immunol. 5, 1-8 (2015). 2.Mkaddem, S.B.,Bens, M. and Vandewalle, A. Differential activation of Toll-like receptor-mediated apoptosis induced by hypoxia. Oncotarget 1(8), 741-750 (2010). 3.Yamada, M.,Ichikawa, T.,Ii, M., et al. Discovery of novel and potent small-molecule inhibitors of NO and cytokine production as antisepsis agents: Synthesis and biological activity of alkyl 6-(N-substituted sulfamoyl)cyclohex-1-ene-1-carboxylate. Journal of Medicinal Chemistry 48(23), 7457-7467 (2005). 4.Ii, M.,Matsunaga, N.,Hazeki, K., et al. 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. Molecular Pharmacology 69(4), 1288-1295 (2006). 5.Matsunaga, N.,Tsuchimori, N.,Matsumoto, T., et al. TAK-242 (resatorvid), a small-molecule inhibitor of Toll-like receptor (TLR) 4 signaling, binds selectively to TLR4 and interferes with interactions between TLR4 and its adaptor molecules. Molecular Pharmacology 79(1), 34-41 (2011). 6.Fenhammar, J.,Rundgren, M.,Hultenby, K., et al. Renal effects of treatment with a TLR4-inhibitor in conscious septic sheep. Critical Care 18(5), 1-12 (2014). 7.Li, X.Q.,Lv, H.W.,Tan, W.F., et al. Role of the TLR4 pathway in blood-spinal cord barrier dysfunction during the bimodal stage after ischemia/reperfusion injury in rats. Journal of Neuroinflammation 11, 1-11 (2014). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 361.8 |
| 分子式 | C15H17NO4ClFS |
| CAS号 | 243984-11-4 |
| 稳定性 | ≥ 2 years |
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