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Cat. No. M4838
TAK-242 Structure


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Biological Activity

TAK-242 (Resatorvid) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling. TAK-242 inhibits the production of lipopolysaccharide-induced inflammatory mediators by binding to the intracellular domain of TLR4. TAK-242 also inhibited mRNA expression of IL-6 and TNF-alpha induced by LPS and interferon-gamma in RAW264.7 cells. TAK-242 suppressed the production of these cytokines from LPS-stimulated human peripheral blood mononuclear cells (PBMCs) at IC50 values from 11 to 33 nM. Intravenous administration of TAK-242 to mice 1 h before LPS challenge dose-dependently inhibited LPS-induced increases in serum levels of TNF-alpha, IL-1beta, IL-6, IL-10, MIP-2, and NO metabolites. TAK-242 protected mice from LPS-induced lethality in a similar dose-dependent manner, and rescued 100% of mice at a dose of 1 mg/kg.

Product Citations
Customer Product Validations & Biological Datas
Source Oncotarget (2018). Figure 3. TAK-242
Method Western blotting
Cell Lines RA-FLS cells
Concentrations -
Incubation Time 24, 48 and 72 h.
Results As shown in Figure 3, the protein and mRNA expressions of TLR4 and NF-κB decreased in the miR-146a mimic and the Tak-242 groups, while mRNA and protein expressions of TLR4 and NF- κB increased in the miR-146a inhibitor and the TLR4 groups, and the mRNA and protein expressions of TLR4 and NF-κB in the TLR4 group were significantly higher than those in the miR-146a inhibitor group
Cell Experiment
Cell lines L6-GLUT4myc
Preparation method Prior to treatment with LPS or stearate, cells were pre-treated with TAK-242 (1 μM) or vehicle control for 1 h. TAK-242 remained in culture medium for the duration for the experiment.
Concentrations 1 μM
Incubation time 1 h
Animal Experiment
Animal models C57Bl/6 mice
Formulation 5% DMSO, 5% Tween80
Dosages 3 mg/kg
Administration i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 361.82
Formula C15H17ClFNO4S
CAS Number 243984-11-4
Purity >98%
Solubility DMSO 10 mg/mL
Storage at -20°C

Systemic TAK-242 prevents intrathecal LPS evoked hyperalgesia in male, but not female mice and prevents delayed allodynia following intraplantar formalin in both male and female mice: The role of TLR4 in the evolution of a persistent pain state
Woller SA, et al. Brain Behav Immun. 2016 Aug;56:271-80. PMID: 27044335.

TAK-242, a small-molecule inhibitor of Toll-like receptor 4 signalling, unveils similarities and differences in lipopolysaccharide- and lipid-induced inflammation and insulin resistance in muscle cells.
Hussey SE, et al. Biosci Rep. 2012 Nov 30;33(1):37-47. PMID: 23050932.

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Keywords: TAK-242, Resatorvid supplier, TLR, inhibitors

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