TAK-242CAS号: 243984-11-4分子式: C15H17ClFNO4S分子量: 361.82描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
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. |
纯度 |
>98%
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储存/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.
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基本信息 | |
别名 |
瑞沙托维; Resatorvid; TAK242; TAK 242
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外观 |
淡黄色固体
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可溶性/溶解性 |
DMSO : ≥ 360 mg/mL (994.97 mM)
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生物活性 | |
靶点 |
TLR4
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In vitro(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.
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In vivo(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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分子结构图