TAK-242 (Resatorvid) 别名：Resatorvid; CLI-095; 瑞沙托维

目录号 M4838

TAK-242 (Resatorvid，瑞沙托维)是一种TLR4信号通路抑制剂，能通过结合TLR4胞内区域，抑制脂多糖LPS诱导的炎症介质的产生。

CAS No.：243984-11-4

规格	价格	库存状态
Free Sample (0.5-1 mg)	¥ 0	现货
2mg	¥ 630	现货
5mg	¥ 1000	现货
10mg	¥ 1600	现货
25mg	¥ 3402	现货

*AbMole所有产品仅供有资质的科研机构或医药企业进行科学研究或药证申报用途，不能被用于人体和任何其它用途。我们不向任何个人或非科研性质的机构提供产品和服务。

客户使用AbMole的TAK-242 (Resatorvid)发表的文献

Clin Exp Pharmacol Physiol. 2025 Jan;52(1):e70008.

TLR4 Inhibitor TAK-242 Protected Henoch–Schonlein Purpura Nephritis in Rats by Regulating Inflammatory Response and Immune Competence via NF- κB/NLRP3 Signalling

Food and Chemical Toxicology. 2024 May 11.

Lead exposure induces autophagy via TLR4/EEF2 in neurons

Poult Sci. 2024 Oct 24.

Selenomethionine alleviates kidney necroptosis and inflammation by restoring lipopolysaccharide-mediated mitochondrial dynamics imbalance via the TLR4/RIPK3/DRP1 signaling pathway in laying hens

Thromb Res. 2023 Feb;222:49-62.

High mobility group box 1 derived mainly from platelet microparticles exacerbates microvascular obstruction in no reflow

Cell Death Dis. 2023 Sep 21;14(9):619.

Interfering with Rac1-activation during neonatal monocyte-macrophage differentiation influences the inflammatory responses of M1 macrophages

Chem Biodivers. 2023 Jan 18.

Cinnamaldehyde ameliorates dextran sulfate sodium‐induced colitis in mice by modulating TLR4/NF‐κB signaling pathway and NLRP3 inflammasome activation

Front Immunol. 2022 Jul 8;13:901566.

Hepatocyte-Conditional Knockout of Phosphatidylethanolamine Binding Protein 4 Aggravated LPS/D-GalN-Induced Acute Liver Injury via the TLR4/NF-κB Pathway

Animals (Basel). 2021 Dec 1;11(12):3422..

NF-κB–Dependent Snail Expression Promotes Epithelial–Mesenchymal Transition in Mastitis

Clinics (Sao Paulo). 2021 Mar 8;76:e2484.

miR-139-5p protects septic mice with acute lung injury by inhibiting Toll-like receptor 4/Myeloid differentiation factor 88/Nuclear factor-&mac_kgr;B signaling pathway

J Clin Invest. 2020 May 19.

Residual endotoxin induces primary graft dysfunction through ischemia-reperfusion-primed alveolar macrophages

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Mar Drυgs. 2020 Aug 17;18(8):429.

Comparison of Physicochemical Characteristics and Macrophage Immunostimulatory Activities of Polysaccharides from Chlamys farreri

Mar Drυgs. 2020 Oct 28;18(11):538.

Immunostimulatory Effects of Polysaccharides from Spirulina platensis In Vivo and Vitro and Their Activation Mechanism on RAW246.7 Macrophages

Biochem Biophys Res Commun. 2020 Oct 22;531(4):602-608.

Toll-like receptor 4 plays a key role in advanced glycation end products-induced M1 macrophage polarization

Cell Mol Neurobiol. 2019 Mar;39(2):301-319.

Myosin IIA Regulated Tight Junction in Oxygen Glucose-Deprived Brain Endothelial Cells Via Activation of TLR4/PI3K/Akt/JNK1/2/14-3-3ε/NF-κB/MMP9 Signal Transduction Pathway.

质量标准及产品资料

纯度：99.91%
COA
H-NMR
HPLC

化学性质/溶解性/储存

分子量	361.82
分子式	C15H17ClFNO4S
CAS号	243984-11-4
中文名称	瑞沙托维
溶解性	DMSO 80 mg/mL
储存条件	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月
运输方式	冰袋运输，根据产品的不同，可能会有相应调整。

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.

实验参考

蛋白/细胞实验

下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。

浓度/溶剂体积/质量	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

*吸湿的DMSO对产品的溶解度有显著影响，请使用新开封的DMSO；
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

质量		浓度		体积		分子量*
	=		x		x

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

* 上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

动物实验

建议您制定动物给药及实验方案时，尽量参考已发表的相关实验文献（溶剂种类及配比众多，简单地溶解目的化合物，并不能解决动物给药依从性、体内生物利用度、组织分布等相关问题，未必能保证目的化合物在动物体内充分发挥生物学效用）。
体内实验的工作液，建议您现用现配，当天使用；如在配制过程中出现沉淀、析出现象，可以通过超声和（或）加热的方式助溶。
切勿一次性将产品全部溶解。