Resatorvid (TAK-242)

Catalog No.S7455

Resatorvid (TAK-242) Chemical Structure

Molecular Weight(MW): 361.82

Resatorvid (TAK-242) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α, IL-6, and IL-1β in macrophages with IC50 values of 1-11 nM.

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Biological Activity

Description Resatorvid (TAK-242) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α, IL-6, and IL-1β in macrophages with IC50 values of 1-11 nM.
Targets
TLR4 [1]
()
In vitro

TAK-242 inhibits the TLR4 pathway by binding directly to a Cys747 in the intracellular TLR4 domain. TAK-242 disrupts the interactions of TLR4 with its adaptor molecules, TIRAP and TRAM[1].

Assay
Methods Test Index PMID
Western blot
TLR4 / p-p65 / p65 / pIκBα / IκBα ; 

PubMed: 29207635     


Non-transfected or transfected (pcDNA or pcDNA-SOCS2) podocytes were pretreated with or without 1 μM TAK-242 for 2 h, and then stimulated with 30 mM glucose for 24 h. Western blot was then performed to detect the levels of TLR4, p-p65, p65, p-IκBα and IκBα in treated podocytes.

Bcl-2 / Cleaved caspase-3 ; 

PubMed: 29207635     


Non-transfected or transfected (pcDNA or pcDNA-SOCS2) podocytes were pretreated with or without 1 μM TAK-242 for 2 h, and then stimulated with 30 mM glucose for 24 h. The levels of Bcl-2 and Cleaved caspase-3 in treated podocytes were examined by western blot.

29207635
Immunofluorescence
TLR4 ; 

PubMed: 29311802     


Immunolabeling and confocal imaging analysis (D) showed elevated TLR4 expression in the cells treated with METH compared with controls. 

NFκB; 

PubMed: 29311802     


Immunolabeling and confocal imaging analysis (D) showed elevated NF-κB expression in the METH-treated cells compared with controls. 

29311802
In vivo

TAK-242 protects against acute cerebral ischemia/reperfusion injury in mice by dose of 3 mg/kg[1]. Topical resatorvid can block UV-induced AP-1 activation in mouse epidermis. In a UV-induced skin tumorigenesis model, topical resatorvid displays potent photochemopreventive activity, significantly suppressing tumor area and multiplicity. Tumors harvested from resatorvid-treated mice display reduced activity of UV-associated signaling pathways and a corresponding increase in apoptosis compared to tumors from control animals[2]. TAK-242 significantly reduces the neuronal damage occurring after cerebral ischemia, a form of stroke in mice[3].

Protocol

Cell Research:

[4]

+ Expand
  • Cell lines: Primary human keratinocytes
  • Concentrations: 10 µM
  • Incubation Time: 6 h
  • Method:

    NF-κB keratinocytes are treated with UVB +/− 10 µM resatorvid (or vehicle) and harvested 6 hr later. Resatorvid significantly inhibits UV-induced NF-κB luciferase signaling in keratinocytes.


    (Only for Reference)
Animal Research:

[3]

+ Expand
  • Animal Models: male ddY mice aged 4-5weeks
  • Formulation: 10% DMSO
  • Dosages: 1 μl (at 0.001, 0.03, or 0.01 μg/μl)
  • Administration: intracerebroventricularly
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 72 mg/mL (198.99 mM)
Ethanol 72 mg/mL (198.99 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 361.82
Formula

C15H17ClFNO4S

CAS No. 243984-11-4
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID