A cell-permeable inhibitor of TLR4 signaling

TAK-242 – 25 mg

Brand:
Cayman
CAS:
243984-11-4
Storage:
-20
UN-No:
Non-Hazardous - /

Toll-like receptor 4 (TLR4) is activated by lipopolysaccharide (LPS), with LPS-binding protein, to initiate an innate immune response.{28195} Alternatively, hypoxia or ischemia/reperfusion can trigger signaling through TLR4.{28194} 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.{28192,28174} It does not affect signaling through other TLRs.{28192,28174,28193} 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.{28192} Mechanistically, TAK-242 acts by selectively binding TLR4 and preventing its association with adaptor proteins that are essential for signal transduction.{28193} TAK-242 is used to study signaling through TLR4 in a variety of pathologies, including sepsis and ischemia/reperfusion injury.{28191,28173}  

 

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Description

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; effective in vivo, suppressing the production of NO, TNF-α, IL-6, and IL-1β in mice treated with LPS when given intravenously

Formal name: 6R-[[(2-chloro-4-fluorophenyl)amino]sulfonyl]-1-cyclohexene-1-carboxylic acid, ethyl ester

Synonyms:  Resatorvid

Molecular weight: 361.8

CAS: 243984-11-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation|Innate Immunity|Pattern Recognition||Research Area|Immunology & Inflammation|Innate Immunity|Sepsis/Shock

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