TAK-242 ≥98%
Leverantör: Cayman Chemical
Synonyms:
Resatorvid, (R)-Ethyl 6-(N-(2-chloro-4-fluorophenyl)sulphamoyl)cyclohex-1-enecarboxylate, 6R-[[(2-chloro-4-fluorophenyl)amino]sulphonyl]-1-cyclohexene-1-carboxylic acid, ethyl ester
Toll-like receptor 4 (TLR4) is activated by lipopolysaccharide (LPS), with LPS-binding protein, to initiate an innate immune response. Alternatively, hypoxia or ischemia/reperfusion can trigger signaling through TLR4. 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. 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. TAK-242 is used to study signaling through TLR4 in a variety of pathologies, including sepsis and ischemia/reperfusion injury.
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Formel:
C₁₅H₁₇NO₄ClFS MW: 361,8 g/mol |
MDL Number:
MFCD11046362 CAS nummer: 243984-11-4 |
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