Resatorvid (TAK-242)

Catalog No.S7455 Batch:S745502

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Technical Data

Formula

C15H17ClFNO4S
Molecular Weight 361.82 CAS No. 243984-11-4
Solubility (25°C)* In vitro DMSO 72 mg/mL (198.99 mM)
Ethanol 72 mg/mL (198.99 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
2%DMSO 98%Corn oil
0.4mg/ml Taking the 1 mL working solution as an example, add 20 μL of 20 mg/ml clear DMSO stock solution to 980 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.1mg/ml Taking the 1 mL working solution as an example, add 50 μL of clarified DMSO stock solution of 102 mg/ml to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Resatorvid (TAK-242, CLI-095) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α and IL-6 in macrophages with IC50 of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy.
Targets
TLR4 [1] IL-6 [5]
(Cell-free assay)		 NO [5]
(Cell-free assay)		 TNF-α [5]
(Cell-free assay)
1.3 nM 1.8 nM 1.9 nM
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].
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 (from reference)

Cell Assay:

[4]
  • 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.
Animal Study:

[3]
  • Animal Models

    male ddY mice aged 4-5weeks

  • Dosages

    1 μl (at 0.001, 0.03, or 0.01 μg/μl)

  • Administration

    intracerebroventricularly

Selleck's Resatorvid (TAK-242) has been cited by 49 publications

Macrophage Tim-3 maintains intestinal homeostasis in DSS-induced colitis by suppressing neutrophil necroptosis [ Redox Biol, 2024, 70:103072] PubMed: 38330550
Fusobacterium nucleatum-triggered neutrophil extracellular traps facilitate colorectal carcinoma progression [ J Exp Clin Cancer Res, 2023, 42(1):236] PubMed: 37684625
Fusobacterium nucleatum-triggered neutrophil extracellular traps facilitate colorectal carcinoma progression [ J Exp Clin Cancer Res, 2023, 42(1):236] PubMed: 37684625
The PTX3/TLR4 autocrine loop as a novel therapeutic target in triple negative breast cancer [ Exp Hematol Oncol, 2023, 12(1):82] PubMed: 37749607
Dual RNA-Sequencing and Liquid Chromatography-Mass Spectrometry Unveil Specific Insights on the Pathogenicity of Trichophyton mentagrophytes Complex [ J Invest Dermatol, 2023, 143(3):470-479.e6] PubMed: 38295003
Extracellular vesicles produced by avian pathogenic Escherichia coli (APEC) activate macrophage proinflammatory response and neutrophil extracellular trap (NET) formation through TLR4 signaling [ Microb Cell Fact, 2023, 22(1):177.] PubMed: 37689682
Extracellular vesicles produced by avian pathogenic Escherichia coli -APEC) activate macrophage proinflammatory response and neutrophil extracellular trap -NET) formation through TLR4 signaling [ Microb Cell Fact, 2023, 22(1):177] PubMed: 37689682
Extracellular vesicles produced by avian pathogenic Escherichia coli (APEC) activate macrophage proinflammatory response and neutrophil extracellular trap (NET) formation through TLR4 signaling [ Microb Cell Fact, 2023, 22(1):177] PubMed: 37689682
Adh Promotes Actinobacillus pleuropneumoniae Survival in Porcine Alveolar Macrophages by Inhibiting CHAC2-Mediated Respiratory Burst and Inflammatory Cytokine Expression [ Cells, 2023, 12(5)696] PubMed: 36899832
Autophagy Activation in Peripheral Blood Mononuclear Cells of Peritoneal Dialysis Patients [ Kidney Int Rep, 2023, 8(9):1852-1863] PubMed: 37705917

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.