TAK-242 | CAS:243984-11-4

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Name:TAK-242; Resatorvid
Cat. No. :CS-0408
CAS No. :243984-11-4
Formula:C15H17ClFNO4S
M. Wt. : 361.82
Solubility:DMSO: ≥ 360 mg/mL

TAK-242 is a potent TLR4 signaling inhibitor, selectively inhibits the TLR4-mediated production of cytokines and NO.IC50 & Target: TLR4[1]In Vitro: In RAW264.7 cells and mouse peritoneal macrophages, TAK-242 suppresses lipopolysaccharide (LPS)-induced production of NO, tumor necrosis factor-α (TNF-α), and interleukin (IL)-6, with IC50 of 1.1 to 11 nM. TAK-242 also suppresses the production of these cytokines from LPS-stimulated human peripheral blood mononuclear cells (PBMCs) at IC50 values from 11 to 33 nM[1].In Vivo: TAK-242 apparently reduces the serum anti-dsDNA levels in both genotype mice. Alternatively, IFN-γ, TNF-α, and IL-1β production is markedly inhibited by TAK-242, but their concentrations are still greatly higher than those in NS-treated counterparts[2]. TAK-242 pre-stress administration prevents the accumulation of potentially deleterious inflammatory and oxidative/nitrosative mediators in the brain frontal cortex of rats. TAK-242 i.v. administration at the beginning of the stress session completely blocks TLR-4 mRNA and protein upregulation after stress exposure[3].

Janda J, et al. Resatorvid-based Pharmacological Antagonism of Cutaneous TLR4 Blocks UV-induced NF-κB and AP-1 Signaling in Keratinocytes and Mouse Skin. Photochem Photobiol. 2016 Nov;92(6):816-825. Wen Z, et al. Positive Feedback Regulation between Transglutaminase 2 and Toll-Like Receptor 4 Signaling in Hepatic Stellate Cells Correlates with Liver Fibrosis Post Schistosoma japonicum Infection. Front Immunol. 2017 Dec 13;8:1808. Gárate I, et al. Toll-like 4 receptor inhibitor TAK-242 decreases neuroinflammation in rat brain frontal cortex after stress. J Neuroinflammation. 2014 Jan 11;11:8. Wang L, et al. Doxorubicin-Induced Systemic Inflammation Is Driven by Upregulation of Toll-Like Receptor TLR4 and Endotoxin Leakage. Cancer Res. 2016 Nov 15;76(22):6631-6642. RAO Xiao-jiao, et al. Effect of TLR4 on expression of inflammatory cytokine in aortic artery in mice with insulin resistance[J]. Chinese Journal of Public Health, 2016, 32(11): 1480-1484. Ii M, et al. A novel cyclohexene derivative, ethyl (6R)-6-[N-(2-Chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate (TAK-242), selectively inhibits toll-like receptor 4-mediated cytokine production through suppression of intracellular signaling. Shibata A, et al. Toll-like receptor 4 antagonist TAK-242 inhibits autoinflammatory symptoms in DITRA. J Autoimmun. 2017 Jun;80:28-38. Ni JQ, et al. Role of toll-like receptor 4 on lupus lung injury and atherosclerosis in LPS-challenge ApoE⁻/⁻ mice. Clin Dev Immunol. 2013;2013:476856.