Resatorvid (TAK-242) - Moligand™, 10mM in DMSO , Antagonist of TLR4, CAS No.243984-11-4, Antagonist of TLR4

CAS: 243984-11-4 Cat. No.: R408997 Molecular Weight: 361.82 EC Number: 897-524-2 PubChem CID: 11703255

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

CLI-095 | 1-​Cyclohexene-​1-​carboxylic acid, 6-​[[(2-​chloro-​4-​fluorophenyl)​amino]​sulfonyl]​-​, ethyl ester, (6R)​-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Resatorvid (TAK-242, CLI-095) is a small-molecule-specific inhibitor ofToll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α and IL-6 in macrophages with IC50 of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulate
In vitro

TAK-242 inhibits the TLR4 pathway by binding directly to a Cys747 in the intracellular TLR4 domain. TAK-242 disrupts the interactions of TLR4 with its adaptor molecules, TIRAP and TRAM.

In vivo

TAK-242 protects against acute cerebral ischemia/reperfusion injury in mice by dose of 3 mg/kg. Topical resatorvid can block UV-induced AP-1 activation in mouse epidermis. In a UV-induced skin tumorigenesis model, topical resatorvid displays potent photochemopreventive activity, significantly suppressing tumor area and multiplicity. Tumors harvested from resatorvid-treated mice display reduced activity of UV-associated signaling pathways and a corresponding increase in apoptosis compared to tumors from control animals. TAK-242 significantly reduces the neuronal damage occurring after cerebral ischemia, a form of stroke in mice.
Cell Data

cell lines：

Concentrations：10 µM

Incubation Time：6 h

Powder Purity:≥99%

Specifications

Synonyms

CLI-095 | 1-​Cyclohexene-​1-​carboxylic acid, 6-​[[(2-​chloro-​4-​fluorophenyl)​amino]​sulfonyl]​-​, ethyl ester, (6R)​-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Resatorvid (TAK-242, CLI-095) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α and IL-6 in macrophages with IC50 of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulat

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

ANTAGONIST

Mechanism of action

Antagonist of TLR4

Product Properties

• ALogP: 3

Names and Identifiers

• Isomeric SMILES: CCOC(=O)C1=CCCC[C@H]1S(=O)(=O)NC2=C(C=C(C=C2)F)Cl
• Alternate CAS: 243984-11-4
• PubChem CID: 11703255
• MeSH Entry Terms: CLI 095;CLI-095;CLI095;ethyl (6R)-6-(N-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-ene-1-carboxylate;ethyl 6-(N-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-ene-1-carboxylate;ethyl CFSCC;resatorvid;TAK 242;TAK-242;TAK242
• Molecular Weight: 361.82

Associated Targets(Human)

TLR4 Tchem Toll-like receptor 4 (0 Activities)

Discover Target: TLR4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 64 mg/mL (199.78 mM); Ethanol: 5 mg/mL (15.6 mM); Water: Insoluble

References

1. Ruyi Zhu, Yaling Zhang, Weitai He, Yanan Sun, Xin Zhao, Yaping Yan, Qian Zhang.  (2024)  Wogonoside alleviates microglia-mediated neuroinflammation via TLR4/MyD88/NF-κB signaling axis after spinal cord injury.  EUROPEAN JOURNAL OF PHARMACOLOGY,      [PMID:38636801] [10.1016/j.ejphar.2024.176566]

2. Ailin Yang, Haitao Fan, Yanan Zhao, Xiaonan Chen, Zhixiang Zhu, Xiaojun Zha, Yunfang Zhao, Xingyun Chai, Jun Li, Pengfei Tu, Zhongdong Hu.  (2019)  An immune-stimulating proteoglycan from the medicinal mushroom Huaier up-regulates NF-κB and MAPK signaling via Toll-like receptor 4.  JOURNAL OF BIOLOGICAL CHEMISTRY,  294  (8): (2628-5268).  [PMID:30602571] [10.1074/jbc.RA118.005477]

3. Lihong Liang, Xue Yang, Hao Zeng, Kai Liao, Runze Zhang, Bowen Wang, Jin Yuan.  (2024)  S100A9-TLR4 axis aggravates dry eye through the blockage of autophagy.  EXPERIMENTAL EYE RESEARCH,      [PMID:39151778] [10.1016/j.exer.2024.110052]

4. Zheng Zhang, Tian Zhu, Yang Li, Bin Yu, Haiteng Tao, Haibo Zhao, Bo Cui.  (2025)  Butyrate Regulates Intestinal DNA Virome and Lipopolysaccharide Levels to Prevent High-Fat Diet-Related Liver Damage in Rats.  JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY,      [PMID:40166958] [10.1021/acs.jafc.4c07966]

5. Zuyue Li, Shasha Wang, Mahmoud Abou-Elsoud, Yijie Li, Houchuntai Wang, Meiyu Liu, Wei Hu, Dong Uk Ahn, Xi Huang.  (2025)  Simulated Gastrointestinal Digestion Enhances the Immunomodulatory Activity of Ovalbumin Peptide NVMEERKIK: Mechanistic Insights into TLR4/MAPK/NF-κB Signaling Modulation.  JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY,      [PMID:40229255] [10.1021/acs.jafc.5c00258]

6. Yi-Fang Zhong, Chan Ding, Chun-Ji Yao, Jia-Chun Wang, Min-Qian Feng, Xiao-Xue Gong, Lin Yu, Hua-Dong Xu, Hai-Ling Xia.  (2025)  HMGB1 as a Key Mediator in Malignant Mesothelioma and a Potential Target for Asbestos-Related Cancer Therapy.  Toxics,  13  (6): (448).  [PMID:40559922] [10.3390/toxics13060448]

7. Zhang Jia, Liu Jin, Chen Yuqian, Chen Huan, Meng Yihan, Wang Yan, Qiu Yuanjie, Hu Huizhong, Shi Wenhua, Li Manxiang, Li Man-xiang.  (2026)  Activation of PBK by Gal-3 contributes to pulmonary artery hypertension by promoting PRC1 activation.  RESPIRATORY RESEARCH,      [PMID:41612370] [10.1186/s12931-026-03534-4]

8. Xiangxiang Xu, Xianlan Chen, Jin Wang, Yuhan Liu, Sidra Mustafa, Lu Diao, Rongrong Zhao, Haiyang Chi, Kang Hu, Jiashan Zhu, Jun Zhao, Mi Liu.  (2026)  Redefining Dendritic Cell Vaccines: Synergistically Co-priming DC and B Cells With Nanoparticles Loading Whole Cell Antigens Maximizes the Efficacy of DC Vaccines.  Advanced Science,      [PMID:41671421] [10.1002/advs.202510615]

9. Hui Zhang, Qimei Yun, Zezhou Xu, Yifan Wang, Xianzhi Zhou, Ling Deng, Binsheng He.  (2026)  TAK-242 alleviates neuroinflammation and poststroke cognitive impairment by targeting the TLR4/SYK/NF-κB pathway in a cerebral ischemia/reperfusion rat model.  EUROPEAN JOURNAL OF PHARMACOLOGY,      [PMID:] [10.1016/j.ejphar.2026.178813]