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TAK-242

目录号 M4838 所有产品仅供科研使用,严禁用于人或动物的治疗等任何其他用途,不为任何个人提供产品和服务  


TAK-242 (Resatorvid)是TLR4信号通路抑制剂,能通过结合TLR4胞内区域抑制脂多糖诱导的炎症介质的产生。

TAK-242结构式

别名:Resatorvid

包装 价格 库存状态
5mg 原价 ¥ 1098
促销价 ¥ 1043.1
中国库存现货
其他规格数量报价?

质量控制及产品安全说明书
生物活性

TAK-242 (Resatorvid) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling. TAK-242 inhibits the production of lipopolysaccharide-induced inflammatory mediators by binding to the intracellular domain of TLR4. TAK-242 also inhibited mRNA expression of IL-6 and TNF-alpha induced by LPS and interferon-gamma in RAW264.7 cells. TAK-242 suppressed the production of these cytokines from LPS-stimulated human peripheral blood mononuclear cells (PBMCs) at IC50 values from 11 to 33 nM. Intravenous administration of TAK-242 to mice 1 h before LPS challenge dose-dependently inhibited LPS-induced increases in serum levels of TNF-alpha, IL-1beta, IL-6, IL-10, MIP-2, and NO metabolites. TAK-242 protected mice from LPS-induced lethality in a similar dose-dependent manner, and rescued 100% of mice at a dose of 1 mg/kg.

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)
细胞实验
细胞系 L6-GLUT4myc
方法 Prior to treatment with LPS or stearate, cells were pre-treated with TAK-242 (1 μM) or vehicle control for 1 h. TAK-242 remained in culture medium for the duration for the experiment.
浓度 1 μM
处理时间 1 h
动物实验
动物模型 C57Bl/6 mice
配制 5% DMSO, 5% Tween80
剂量 3 mg/kg
给药处理 i.v.
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
小鼠 大鼠 豚鼠 仓鼠
重量 (kg) 0.02 0.15 1.8 0.4 0.08 10
体表面积 (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km 系数 3 6 12 8 5 20
动物 A (mg/kg) = 动物 B (mg/kg) ×  动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量,需要将22.4 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。

化学数据
分子量 361.82
分子式 C15H17ClFNO4S
CAS号 243984-11-4
纯度 >98%
溶解性(25°C) DMSO 10 mg/mL
储存和运输条件 固体粉末: -20°C 冷藏长期储存
常温运输及临时存放
储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.7638 mL 13.819 mL 27.6381 mL
5 mM 0.5528 mL 2.7638 mL 5.5276 mL
10 mM 0.2764 mL 1.3819 mL 2.7638 mL
使用AbMole产品发表的文献
客户产品验证及相关生物数据
数据来源 Oncotarget (2018). Figure 3. TAK-242
方法 Western blotting
细胞系 RA-FLS cells
浓度 -
处理时间 24, 48 and 72 h.
实验结果 As shown in Figure 3, the protein and mRNA expressions of TLR4 and NF-κB decreased in the miR-146a mimic and the Tak-242 groups, while mRNA and protein expressions of TLR4 and NF- κB increased in the miR-146a inhibitor and the TLR4 groups, and the mRNA and protein expressions of TLR4 and NF-κB in the TLR4 group were significantly higher than those in the miR-146a inhibitor group
参考文献

Systemic TAK-242 prevents intrathecal LPS evoked hyperalgesia in male, but not female mice and prevents delayed allodynia following intraplantar formalin in both male and female mice: The role of TLR4 in the evolution of a persistent pain state
Woller SA, et al. Brain Behav Immun. 2016 Aug;56:271-80. PMID: 27044335.

TAK-242, a small-molecule inhibitor of Toll-like receptor 4 signalling, unveils similarities and differences in lipopolysaccharide- and lipid-induced inflammation and insulin resistance in muscle cells.
Hussey SE, et al. Biosci Rep. 2012 Nov 30;33(1):37-47. PMID: 23050932.

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关键词:TAK-242, Resatorvid, TAK-242供应商, TLR抑制剂, 购买TAK-242, TAK-242结构式

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