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  6. TAK-242; CLI-095

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Supplier NameMedChemExpress (MCE)
Contactsales
Tel609-228-6898
Mobile609-228-6898
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Emailsales@medchemexpress.com; tech@medchemexpress.com
Websitehttp://www.medchemexpress.com/
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Product NameRESATORVID
SynonymsTAK 242
RESATORVID
Resatorvid(TAK-242)
TAK-242(Resatorvid)
(R)-ethyl 6-(N-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-enecarboxylate
(6R)-6-[[(2-Chloro-4-fluorophenyl)amino]sulfonyl]-1-cyclohexene-1-carboxylic acid ethyl ester

Synonyms

TAK 242
RESATORVID
Resatorvid(TAK-242)
TAK-242(Resatorvid)
(R)-ethyl 6-(N-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-enecarboxylate
(6R)-6-[[(2-Chloro-4-fluorophenyl)amino]sulfonyl]-1-cyclohexene-1-carboxylic acid ethyl ester
Cyclohexene-1-carboxylic acid, 6-[[(2-chloro-4-fluorophenyl)amino]sulfonyl]-, ethyl ester, (6R)-
1-Cyclohexene-1-carboxylic acid, 6-[[(2-chloro-4-fluorophenyl)aMino]sulfonyl]-, ethyl ester, (6R)-
CAS243984-11-4
EINECS
Chemical FormulaC15H17ClFNO4S
Molecular Weight361.82
inchi
Package10 mM * 1 mL;5 mg;10 mg;50 mg
PriceEmail to quote
DescriptionsResatorvid

Resatorvid

MedChemExpress (MCE)

HY-11109

243984-11-4

TAK-242

Descriptions

Resatorvid

Resatorvid

MedChemExpress (MCE)

HY-11109

243984-11-4

TAK-242
CLI-095

99.10%

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

Room temperature in continental US
may vary elsewhere.

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.

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].

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].

TLR4 TNF-R 1.9 nM (IC50) IL-6 1.3 nM (IC50)

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[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. [Content Brief]

[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.
[Content Brief]

[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.
[Content Brief]

Supplier Websitehttp://www.medchemexpress.com/TAK-242.html
Last Update2025-10-14 16:03:33
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