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TAK-242

(Synonyms: 瑞沙托维; TAK-242; CLI-095)

目录号: PC11537 纯度: ≥98%

TLR 4信号抑制剂,Resatorvid (TAK-242) 是一种有效的 TLR4 信号传导抑制剂，可选择性地抑制TLR-介导的细胞因子和一氧化氮的产生。

CAS No. :243984-11-4

商品编号	规格	价格	会员价
PC11537-5mg	5mg	¥777.00	请登录
PC11537-10mg	10mg	¥1175.00	请登录
PC11537-50mg	50mg	¥8918.00	请登录
PC11537-100mg	100mg	¥7025.00	请登录
PC11537-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥1681.00	请登录

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中文名称

TAK-242

中文别名

瑞沙托维

英文名称

TAK-242

英文别名

Resatorvid;TAK-242;tak242;TAK-242 (CLI-095,Resatorvid);TAK-242(Resatorvid);(6R)-6-[[(2-Chloro-4-fluorophenyl)amino]sulfonyl]-1-cyclohexene-1-carboxylic acid ethyl ester;H2MZ648C31;Resatorvid [INN];C15H17ClFNO4S;GTPL9036;ethyl 6-[(2-chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate;BDBM50155929;4003AH;A3850;P111021;ethyl (6R)-6-[(2-chloro-4-fluorophenyl)sulfamoyl]cyclohexene-1-carboxylate;ethyl (6r)-6-[n-(2-chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate;ethyl (6R)-

Cas No.

243984-11-4

分子式

C₁₅H₁₇ClFNO₄S

分子量

361.82

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

详情描述

TLR 4信号抑制剂,Resatorvid (TAK-242) 是一种有效的 TLR4 信号传导抑制剂，可选择性地抑制TLR-介导的细胞因子和一氧化氮的产生。

生物活性

Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor. Resatorvid inhibits NO, TNF-α and IL-6 production with IC_50s of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy and plays pivotal role in various inflammatory diseases.

性状

Solid

IC50 & Target[1][2]

TLR4

IL-6

1.3 nM (IC₅₀)

TNF-R

1.9 nM (IC₅₀)

体外研究(In Vitro)

Resatorvid suppresses the production of NO, TNF-α, and IL-6 from LPS-stimulated human peripheral blood mononuclear cells (PBMCs) at IC₅₀ values from 11 to 33 nM.
Resatorvid (1-100 nM; 4 hours) inhibits mRNA expression of IL-6 and TNF-α induced by LPS and IFN-γ in RAW264.7 cells.
Resatorvid (1-100 nM; 15 minutes; PBMCs cells) markedly inhibits the LPS-induced phosphorylation of extracellular signal-regulated kinase 1/2 (Erk1/2), p38, and JNK/SAPK as well as degradation of IκBβ at a concentration of 100 nM.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR

Cell Line:	RAW264.7 cells
Concentration:	1 nM, 10 nM, 100 nM
Incubation Time:	4 hours
Result:	TNF-α and IL-6 mRNA expression levels were clearly suppressed at concentrations of 10 to 100 nM.

Western Blot Analysis

Cell Line:	PBMCs cells
Concentration:	1 nM, 10 nM, 100 nM
Incubation Time:	15 minutes
Result:	The phosphorylation of mitogen-activated protein kinases induced by LPS was also inhibited in a concentration-dependent manner.

体内研究(In Vivo)

Resatorvid (TAK-242; 3?mg/kg; intraperitoneal injection; for 2 days; male C57BL/6 mice) pretreatment markedly and significantly reverses the LPS-induced body weight loss, TA muscle loss, and muscle strength loss. TAK-242 reverses the LPS-induced shrinkage of muscle fibres and increases the interstitial space. TAK-242 blocks systemic catabolic cytokine release and skeletal muscle proteolysis in LPS-administered mice.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male C57BL/6 mice (8-12 weeks of age) treated with lipopolysaccharide (LPS)
Dosage:	3?mg/kg
Administration:	Intraperitoneal injection; for 2 days
Result:	Pretreatment of mice reduced or reversed all the detrimental effects of LPS.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. 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. [Information]

[2]. Yamada M, et al. Discovery of novel and potent small-molecule inhibitors of NO and cytokine production as antisepsis agents: synthesis and biological activity of alkyl 6-(N-substituted sulfamoyl)cyclohex-1-ene-1-carboxylate. J Med Chem. 2005 Nov 17;48(23) [Information]

[3]. Yuko Ono, et al. TAK-242, a Specific Inhibitor of Toll-like Receptor 4 Signalling, Prevents Endotoxemia-Induced Skeletal Muscle Wasting in Mice. Sci Rep. 2020 Jan 20;10(1):694. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (276.38 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7638 mL	13.8190 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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: 5.5 mg/mL (15.20 mM); Suspended solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: 5.5 mg/mL (15.20 mM); Suspended solution; Need ultrasonic
3.

建议依照次序添加每种溶剂： 10% DMSO 90% saline
Solubility: 5 mg/mL (13.82 mM); Suspended solution; Need ultrasonic
4.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.75 mg/mL (7.60 mM); Clear solution

此方案可获得 ≥ 2.75 mg/mL (7.60 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
5.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.75 mg/mL (7.60 mM); Suspended solution; Need ultrasonic

此方案可获得 2.75 mg/mL (7.60 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
6.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.75 mg/mL (7.60 mM); Clear solution

此方案可获得 ≥ 2.75 mg/mL (7.60 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
7.

建议依照次序添加每种溶剂： 5% DMSO 95% saline
Solubility: 2.5 mg/mL (6.91 mM); Suspended solution; Need ultrasonic
8.

建议依照次序添加每种溶剂： 1% DMSO 99% saline
Solubility: 0.5 mg/mL (1.38 mM); Suspended solution; Need ultrasonic

搜索质检报告(COA)

产品使用指南

Data Sheet

[1]. 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. [Information]

[2]. Yamada M, et al. Discovery of novel and potent small-molecule inhibitors of NO and cytokine production as antisepsis agents: synthesis and biological activity of alkyl 6-(N-substituted sulfamoyl)cyclohex-1-ene-1-carboxylate. J Med Chem. 2005 Nov 17;48(23) [Information]

[3]. Yuko Ono, et al. TAK-242, a Specific Inhibitor of Toll-like Receptor 4 Signalling, Prevents Endotoxemia-Induced Skeletal Muscle Wasting in Mice. Sci Rep. 2020 Jan 20;10(1):694. [Information]

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

TAK-242

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