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

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Resatorvid (Synonyms: 瑞沙托维; TAK-242; CLI-095) 纯度: 99.72%

Resatorvid (TAK-242) 是一种选择性的 TLR4 信号传导抑制剂。Resatorvid 抑制 NOTNF-αIL-6 的产生,其 IC50 值分别为 1.8 nM,1.9 nM,1.3 nM。Resatorvid 下调 TLR4 下游信号分子 MyD88 和 TRIF 的表达。Resatorvid 抑制自噬 (autophagy),并在各种炎症性疾病中起关键作用。

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

Resatorvid Chemical Structure

CAS No. : 243984-11-4

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1210 In-stock
5 mg ¥1100 In-stock
10 mg ¥1700 In-stock
50 mg ¥7000 In-stock
100 mg ¥12000 In-stock
200 mg ¥21000 In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Resatorvid 相关产品

相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • CNS-Penetrant Compound Library
  • Autophagy Compound Library
  • Small Molecule Immuno-Oncology Compound Library
  • Drug Repurposing Compound Library
  • Antioxidants Compound Library
  • Differentiation Inducing Compound Library
  • Oxygen Sensing Compound Library
  • Pyroptosis Compound Library
  • Anti-Obesity Compound Library
  • Angiogenesis Related Compound Library
  • Rare Diseases Drug Library

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 IC50s 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[1][2].

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[1].
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[1].
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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR[1]

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[1]

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[3].

上海金畔生物科技有限公司 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)[3]
Dosage: 3 mg/kg
Administration: Intraperitoneal injection; for 2 days
Result: Pretreatment of mice reduced or reversed all the detrimental effects of LPS.

Clinical Trial

分子量

361.82

Formula

C15H17ClFNO4S

CAS 号

243984-11-4

中文名称

瑞沙托维

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

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

配制储备液
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

*

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
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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.

    请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: 5.5 mg/mL (15.20 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: 5.5 mg/mL (15.20 mM); Suspended solution; Need ultrasonic

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% saline

    Solubility: 5 mg/mL (13.82 mM); Suspended solution; Need ultrasonic

  • 4.

    请依序添加每种溶剂: 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 ddH₂O 中,得到澄清透明的生理盐水溶液

  • 5.

    请依序添加每种溶剂: 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.

    请依序添加每种溶剂: 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.

    请依序添加每种溶剂: 5% DMSO   95% saline

    Solubility: 2.5 mg/mL (6.91 mM); Suspended solution; Need ultrasonic

  • 8.

    请依序添加每种溶剂: 1% DMSO    99% saline

    Solubility: 0.5 mg/mL (1.38 mM); Suspended solution; Need ultrasonic

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

    [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):7457-67.

    [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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务