For research use only.
Catalog No.S7455 Synonyms: CLI-095
CAS No. 243984-11-4
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.
Selleck's Resatorvid (TAK-242) has been cited by 12 publications
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|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.|
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.
TAK-242 protects against acute cerebral ischemia/reperfusion injury in mice by dose of 3 mg/kg. 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. TAK-242 significantly reduces the neuronal damage occurring after cerebral ischemia, a form of stroke in mice.
-  Kuzmich NN, et al. Vaccines (Basel). 2017, 5(4). pii: E34.
-  Blohm-Mangone K, et al. Cancer Prev Res (Phila). 2018, 11(5):265-278.
-  Suzuki Y, et al. Sci Rep. 2012, 2:896.
|In vitro||DMSO||72 mg/mL (198.99 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04620148||Not yet recruiting||Drug: TAK-242|Drug: Placebo||Acute-On-Chronic Liver Failure||Akaza Bioscience Ltd|Iqvia Pty Ltd||December 2021||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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