Resatorvid (TAK-242)

Catalog No.S7455 Batch:S745501

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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
* <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 57 publications

Identification of hypoxic macrophages in glioblastoma with therapeutic potential for vasculature normalization [ Cancer Cell, 2024, S1535-6108(24)00119-3] PubMed: 38640932
IL36G-producing neutrophil-like monocytes promote cachexia in cancer [ Nat Commun, 2024, 15(1):7662] PubMed: 39266531
Macrophage Tim-3 maintains intestinal homeostasis in DSS-induced colitis by suppressing neutrophil necroptosis [ Redox Biol, 2024, 70:103072] PubMed: 38330550
Streptococcus pneumoniae endopeptidase O induces trained immunity and confers protection against various pathogenic infections [ Clin Immunol, 2024, 263:110226] PubMed: 38663493
Treg and neutrophil extracellular trap interaction contributes to the development of immunosuppression in sepsis [ JCI Insight, 2024, e180132] PubMed: 38888975
Suppressing neutrophil itaconate production attenuates Mycoplasma pneumoniae pneumonia [ PLoS Pathog, 2024, 20(11):e1012614] PubMed: 39499730
Peripheral inflammation triggering central anxiety through the hippocampal glutamate metabolized receptor 1 [ CNS Neurosci Ther, 2024, 30(4):e14723] PubMed: 38676295
Peripheral inflammation triggering central anxiety through the hippocampal glutamate metabolized receptor 1 [ CNS Neurosci Ther, 2024, 30(4):e14723] PubMed: 38676295
Hangeshashinto Inhibits Porphyromonas gingivalis Pathogen-Associated Molecular Patterns-Mediated IL-6 and IL-8 Production through Toll-Like Receptors in CAL27 Cells [ Evid Based Complement Alternat Med, 2024, 2024:9866670] PubMed: 38665937
Fusobacterium nucleatum-triggered neutrophil extracellular traps facilitate colorectal carcinoma progression [ J Exp Clin Cancer Res, 2023, 42(1):236] PubMed: 37684625

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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.

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