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resatorvid

别名	TAK242, TAK-242
Compound Class	Synthetic organic
变动原因	Resatorvid (TAK242) was first identified as an inhibitor of inflammatory mediator production in LPS treated mouse macrophages . Subsequent work found that this action was attributable to the compound's activity as a Toll-like receptor 4 (TLR4) antagonist .
Related Product	TAK-242,TLR4信号传导抑制剂

Summary

是否批准为药物？
IUPAC Name	ethyl (6R)-6-[(2-chloro-4-fluorophenyl)sulfamoyl]cyclohexene-1-carboxylate
别名	TAK242, TAK-242

数据库链接

PubChem CID	11703255
ChEMBL Ligand	CHEMBL225157

生物活性

生物活性评价	In vitro, resatorvid inhibits cytokine production in human PBMCs without antagonizing the binding of LPS to the CD14/TLR4/MD-2 complex . Resatorvid inhibits cytokine production from mouse RAW264.7 cells stimulated with various TLR4 agonists, but not TRL2, -3 or -9 agonists, confirming it as a selective TLR4 antagonist . The Ii et al. paper does not provide binding assay-derived data quantifying TLR4-resatorvid antagonism, all confirmatory work involved measuring inhibition of agonist-induced cytokine expression or secretion. We have tagged TLR4 as the primary molecular target for resatorvid based on this study.
关联靶标	TLR4

临床资料

Summary of Clinical Use	Resatorvid failed Phase 3 clinical trials as a treatment for sepsis (see NCT00633477 and NCT00143611).
作用机制与药效学效应	Sulfonamides are structural analogues of 4-aminobenzoic acid (pABA) an intermediate in the de novo synthesis of folate by some prokaryotes, lower eukaryotes and plants . The antibacterial MMOA is competitive inhibition of bacterial dihydropteroate synthase (DHPS) resulting in a block of folate biosynthesis .

参考文献

1. Yamada M, Ichikawa T, Ii M, Sunamoto M, Itoh K, Tamura N, Kitazaki T. (2005) 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, 48 (23): (7457-67). [PMID:16279805]
2. Ii M, Matsunaga N, Hazeki K, Nakamura K, Takashima K, Seya T, Hazeki O, Kitazaki T, Iizawa Y. (2006) 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.. Mol Pharmacol, 69 (4): (1288-95). [PMID:16373689]

结构

Canonical SMILES	CCOC(=O)C1=CCCCC1S(=O)(=O)Nc1ccc(cc1Cl)F
Isomeric SMILES	CCOC(=O)C1=CCCC[C@H]1S(=O)(=O)Nc1ccc(cc1Cl)F
InChI	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
InChI key	LEEIJTHMHDMWLJ-CQSZACIVSA-N

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