Resatorvid

Chemical compound From Wikipedia, the free encyclopedia

Resatorvid (TAK-242) is a cyclohexane derivative that was invented by scientists at Takeda in a drug discovery campaign to identify inhibitors of the receptor TLR4.[1] It binds directly to cysteine residue 747[1] intracellularly, preventing TLR4 binding with TIRAP and thus preventing downstream signal transduction.[2]

Trade namesResatorvid
CAS Number
Quick facts Clinical data, Trade names ...
Resatorvid
Clinical data
Trade namesResatorvid
Identifiers
  • ethyl (6R)-6-[(2-chloro-4-fluorophenyl)sulfamoyl]cyclohexene-1-carboxylate
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC15H17ClFNO4S
Molar mass361.81 g·mol−1
3D model (JSmol)
  • CCOC(=O)C1=CCCC[C@H]1S(=O)(=O)NC2=C(C=C(C=C2)F)Cl
  • InChI=1S/C15H17ClFNO4S/c1-2-22-15(19)11-5-3-4-6-14(11)23(20,21)18-13-8-7-10(17)9-12(13)16/h5,7-9,14,18H,2-4,6H2,1H3/t14-/m1/s1
  • Key:LEEIJTHMHDMWLJ-CQSZACIVSA-N
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A randomized, double-blinded Phase III trial of resatorvid in sepsis was halted early due to lack of efficacy, and the compound has become a widely used tool compound in biological research.[1]

It has antiinflammatory and neuroprotective effects in preclinical models.[3] It has been explored in preclinical studies of several forms of cancer, including multiple myeloma, breast cancer, and ovarian cancer,[4] and has been suggested for study in skin cancers.[5]

Efforts have been made to improve resatorvid by making prodrugs and deuterated derivatives.[3]

See also

References

Further reading

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