Home Immunology & Inflammation TLR inhibitor - TNF-alpha inhibitor - Autophagy inhibitor - Interleukins inhibitor - MyD88 inhibitor - TRIF inhibitor Resatorvid (TAK-242) For research use only.

Resatorvid (TAK-242)

Synonyms: CLI-095

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.

Resatorvid (TAK-242) Chemical Structure

Resatorvid (TAK-242) Chemical Structure

CAS No. 243984-11-4

Purity & Quality Control

Resatorvid (TAK-242) Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RAW264.7 Function assay Inhibition of LPS-induced IL6 production in mouse RAW264.7 cells by ELISA, IC50 = 0.0013 μM. 16279805
RAW264.7 Function assay Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells, IC50 = 0.0018 μM. 16279805
RAW264.7 Function assay Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells by ELISA, IC50 = 0.0019 μM. 16279805
HEK-Blue Function assay 2 hrs Inhibition of human TLR4 signaling expressed in HEK-Blue cells co-expressing MD2/CD14 assessed as reduction in LPS-induced NF-kappaB activation-mediated SEAP production preincubated for 2 hrs followed by LPS stimulation for 20 hrs by colorimetric assay, IC50 = 0.68 μM. 29472126
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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
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].
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot TLR4 / p-p65 / p65 / pIκBα / IκBα Bcl-2 / Cleaved caspase-3 29207635
Immunofluorescence TLR4 NFκB 29311802
In Vivo
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].
Animal Research Animal Models male ddY mice aged 4-5weeks
Dosages 1 μl (at 0.001, 0.03, or 0.01 μg/μl)
Administration intracerebroventricularly
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04620148 Unknown status
Acute-On-Chronic Liver Failure
Akaza Bioscience Ltd|Iqvia Pty Ltd
 December 2021 Phase 2

Chemical Information & Solubility

Molecular Weight 361.82 Formula

C15H17ClFNO4S
CAS No. 243984-11-4 SDF --
Smiles CCOC(=O)C1=CCCCC1S(=O)(=O)NC2=C(C=C(C=C2)F)Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 72 mg/mL ( (198.99 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 72 mg/mL

Water : Insoluble


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