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)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 5.100mg/ml (14.10mM) 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. 
Clear solution
2%DMSO 98%Corn oil

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 0.400mg/ml (1.11mM) 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. 
* <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

References

  • https://pubmed.ncbi.nlm.nih.gov/28976923/
  • https://pubmed.ncbi.nlm.nih.gov/29437671/
  • https://pubmed.ncbi.nlm.nih.gov/23193438/
  • https://www.ncbi.nlm.nih.gov/pubmed/?term=27859308
  • https://pubmed.ncbi.nlm.nih.gov/16279805/

Selleck's Resatorvid (TAK-242) has been cited by 69 publications

Macrophages form dendrite-like pseudopods to enhance bacterial ingestion [ EMBO J, 2025, 10.1038/s44318-025-00515-z] PubMed: 40721684
Immunostimulatory effects of isomalto/malto-polysaccharides via TLR2 and TLR4 in preventing doxycycline-induced cytokine loss [ Carbohydr Polym, 2025, 350:122980] PubMed: 39647934
α-Synuclein orchestrates Th17 responses as antigen and adjuvant in Parkinson's disease [ J Neuroinflammation, 2025, 22(1):38] PubMed: 39934862
Cycloastragenol reduces inflammation in CLP-induced septic MICE by suppressing TLR4 signaling pathways [ Phytomedicine, 2025, 142:156645] PubMed: 40319834
Sodium butyrate attenuates experimental neonatal necrotizing enterocolitis by suppressing TLR4-mediated NLRP3 inflammasome-dependent pyroptosis [ Food Funct, 2025, 16(9):3508-3524] PubMed: 40223745
Intracellular CIRP promotes liver regeneration via STAT3 signaling pathway activation after partial hepatectomy in mice [ Int J Mol Med, 2025, 55(3)42] PubMed: 39791211
Bone Marrow Myeloid-Lymphatic Progenitors Expand Tumor Lymphatic Vasculature Through Cell Fusion [ Cancers (Basel), 2025, 17(11)1804] PubMed: 40507286
GATA1 Transcriptionally Upregulates LMCD1, Promoting Ferroptosis in Sepsis-Associated Acute Kidney Injury Through the Hippo/YAP Pathway [ Kaohsiung J Med Sci, 2025, e70071.] PubMed: 40650665
Identification of hypoxic macrophages in glioblastoma with therapeutic potential for vasculature normalization [ Cancer Cell, 2024, S1535-6108(24)00119-3] PubMed: 38640932
A conserved pilin from uncultured gut bacterial clade TANB77 enhances cancer immunotherapy [ Nat Commun, 2024, 15(1):10726] PubMed: 39730328

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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.