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TAK-242,TLR4信号传导抑制剂

TLR4信号传导抑制剂
规格或纯度: ≥98%
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TLR4 Antagonist
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基本描述

规格或纯度 ≥98%
英文名称 TAK-242
别名 瑞沙托维；TLR4 抑制剂；乙基-(6R)-6-(N-(2-氯-4-氟苯基)氨磺酰基)环己-1-烯-1-羧酸乙酯
英文别名 Resatorvid;TAK242;TAK 242; Ethyl-(6R)-6-(N-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-ene-1-carboxylate
生化机理 Toll样受体4（TLR4）信号抑制剂。与TLR4的细胞内结构域结合。体外抑制LPS诱导的细胞因子产生（IL-6，TNFα和NO产生的IC50值为1.3、1.3和3.2 nM）。减少脑海绵状畸形（CCM）小鼠模型中的病变体积。当与头孢他啶合用时，还能减轻小鼠败血症模型中增加的细胞因子水平。细胞可渗透。
储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍

TAK-242 是一种有效的 TLR4 抑制剂，选择性抑制 TLR4 调节的细胞因子和 NO 产生。

TAK-242 is a cell-permeable compound that selectively binds to Cys747 of TLR4 and selectively disrupts its interaction with adaptor molecules TIRAP and TRAM.

名称和标识符

IUPAC Name ethyl (6R)-6-[(2-chloro-4-fluorophenyl)sulfamoyl]cyclohexene-1-carboxylate
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
Canonical SMILES CCOC(=O)C1=CCCCC1S(=O)(=O)NC2=C(C=C(C=C2)F)Cl
分子式

C15H17ClFNO4S
关联CAS 243984-11-4
UNII H2MZ648C31
PubChem CID 11703255
分子量 361.82

化学和物理性质

溶解性 溶于DMSO, 最高浓度 (mg/mL): 36.18, 最高浓度(mM): 100；溶于ethanol, 最高浓度 (mg/mL): 36.18, 最高浓度(mM): 100

靶标

Target ID 1754
名称 TLR4
缩写名 SHP2
家族 Toll-like receptor family
别名 MGC21621
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 1 839 9q33.1 TLR4 toll like receptor 4
Mouse 1 835 4 34.66 cM Tlr4 toll-like receptor 4
Rat 1 835 5q24 Tlr4 toll-like receptor 4
Ensembl Gene ENSG00000136869 (Hs) , ENSMUSG00000039005 (Mm) , ENSRNOG00000010522 (Rn)
Entrez Gene 21898 (Mm) , 29260 (Rn) , 7099 (Hs)
Protein GI 19924153 (Hs) , 10946594 (Mm) , 25742799 (Rn)
UniProtKB O00206 (Hs) , Q9QUK6 (Mm) , Q9QX05 (Rn)
CATH/Gene3D 3.40.50.10140 (N/A) , 3.80.10.10 (N/A)
ChEMBL Target CHEMBL4523480 (Rn) , CHEMBL5255 (Hs) , CHEMBL1795167 (Mm)

关联配体

Ligand ID 9036
名称 resatorvid
别名 TAK242
类别 Synthetic organic
学名 ethyl (6R)-6-[(2-chloro-4-fluorophenyl)sulfamoyl]cyclohexene-1-carboxylate
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.
评价 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 .
临床描述 The purpose of this study is to determine the optimal dose of Resatorvid for reducing 28-day all-cause mortality in subjects with severe sepsis.
The purpose of this study is to determine the effect of resatorvid on subjects with sepsis.
来源公司 Takeda
Takeda

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]

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