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抑制剂描述:

产品名称:TAK-242 (Resatorvid)

产品别名:见爱必信官网

英文别名:TAK-242 (Resatorvid)

靶点:TLR

CAS:243984-11-4

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

TAK-242 (Resatorvid), a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, inhibits the production of lipopolysaccharide-induced inflammatory mediators by binding to the intracellular domain of TLR4.

溶解性:DMSO : ≥ 360 mg/mL (994.97 mM)

体外研究:

In RAW264.7 cells and mouse peritoneal macrophages, Resatorvid (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. Resatorvid (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.

体内研究:Resatorvid (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 Resatorvid (TAK-242), but their concentrations are still greatly higher than those in NS-treated counterparts. Resatorvid (TAK-242) pre-stress administration prevents the accumulation of potentially deleterious inflammatory and oxidative/nitrosative mediators in the brain frontal cortex of rats. Resatorvid (TAK-242) i.v. administration at the beginning of the stress session completely blocks TLR-4 mRNA and protein upregulation after stress exposure.

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