614316
TAK-242
≥98% (HPLC), solid, TLR4 inhibitor, Calbiochem®
别名:
TLR4抑制剂，TAK-242, 乙基-(6R)-6-(N-(2-氯-4-氟苯基)氨磺酰基)环己-1-烯-1-羧酸乙酯
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选择尺寸
关于此项目
经验公式（希尔记法）:
C15H17ClFNO4S
化学文摘社编号:
分子量:
361.82
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
产品名称
TLR4抑制剂，TAK-242, TAK-242; CAS 243984-11-4; is a cell-permeable compound that selectively binds to Cys747 of TLR4 and selectively disrupts its interaction with adaptor molecules TIRAP and TRAM.
SMILES string
Fc1cc(c(cc1)N[S](=O)(=O)[C@@H]2CCCC=C2C(=O)OCC)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
InChI key
LEEIJTHMHDMWLJ-CQSZACIVSA-N
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
white to yellow-white
solubility
DMSO: 100 mg/mL
shipped in
wet ice
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
可逆性：是
细胞可渗透性：具有
首要靶标
TLR4
TLR4
Disclaimer
毒性：有害（C）
General description
一种细胞渗透性环己烯羧酸盐，可通过TLR4细胞内Cys747残基选择性的结合TLR4而非TLR1-3或TLR5-10，破坏TLR4与衔接子分子TIRAP和TRAM的相互作用。已显示出可有效抑制TLR4介导的信号转导事件，包括在鼠RAW264.7巨噬细胞中LPS诱导的NO和炎性细胞因子生成（针对NO、IL-6和TNF-α生成的各自IC50 = 1.8，1.3和1.9 nM）、TLR4/TIRAP依赖性NF-κB活性以及在TIRAP或TRAM转染的HEK293-hTLR4/MD2-CD14细胞中的TLR4/TIRAP-和TLR4/TRAM依赖性ISRE活性(IC50<300 nM)。据报道，静脉注射给药3 mg/kg时，TAK-242可完全抑制小鼠体内LPS（7 mg/kg，腹腔注射）诱导的死亡。与头孢他啶（3 mg/kg TAK-242和20 mg/kg头孢他啶，i.v.）共同给药时，因感染性休克而导致的死亡的彻底消除可扩展至活的大肠杆菌感染的小鼠。
Other Notes
Matsunaga, N., et al. 2011.Mol.Pharmacol.79, 34.
Takashima, K., et al. 2009.Br. J. Pharmacol.157, 1250.
Li, M., et al. 2006.Mol.Pharmacol.69, 1288.
Yamada, M., et al. 2005.J. Med. Chem.48, 7457.
Takashima, K., et al. 2009.Br. J. Pharmacol.157, 1250.
Li, M., et al. 2006.Mol.Pharmacol.69, 1288.
Yamada, M., et al. 2005.J. Med. Chem.48, 7457.
Packaging
用惰性气体包装
Preparation Note
在重悬后分装并冻存于冰箱（-70°C）。储备液可在-70°C最长稳定1年。仅使用新鲜的DMSO。
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
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