Resatorvid

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].

Product Specifications

CAS Number

[243984-11-4]

Product Name Alternative

TAK-242; CLI-095

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Autophagy; Interleukin Related; TNF Receptor; Toll-like Receptor (TLR)

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; Immunology/Inflammation

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Cancer

Assay Protocol

https://www.medchemexpress.com/TAK-242.html

Purity

99.95

Solubility

DMSO : 100 mg/mL (ultrasonic) |Ethanol : 20 mg/mL (ultrasonic; warming)

Smiles

O=S([C@H]1C(C(OCC)=O)=CCCC1)(NC2=CC=C(C=C2Cl)F)=O

Molecular Formula

C15H17ClFNO4S

Molecular Weight

361.82

Precautions

H302, H315, H319, H335

References & Citations

[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.