产品说明
一般描述
A cell-permeable cyclohexenecarboxylate that disrupts TLR4 interaction with adaptor molecules TIRAP and TRAM by selectively binding to TLR4, but not TLR1-3 or TLR5-10, via TLR4 intracellular Cys747 residue. Shown to effectively inhibit TLR4-mediated signaling events, including LPS-induced NO and inflammatory cytokines production in murine RAW264.7 macrophages (IC50 = 1.8, 1.3, and 1.9 nM, respectively, against NO, IL-6, and TNF-α production), TLR4/TIRAP-dependent NF-κB activity as well as TLR4/TIRAP- and TLR4/TRAM-dependent ISRE activity (IC50<300 nM) in HEK293-hTLR4/MD2-CD14 transfected with either TIRAP or TRAM. When administered at an i.v. dose of 3 mg/kg, TAK-242 is reported to completely prevent LPS- (7 mg/kg, i.p.) induced death in mice in vivo. Complete elimination of septic shock-induced death can be extended to live E. coli-infected mice when co-administered with ceftazidime (3 mg/kg TAK-242 and 20 mg/kg ceftazidime, i.v.).
生化/生理作用
Cell permeable: yes
Reversible: no
Primary Target
TLR4
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
外形
A 25 mM (2 mg/221 µL) sterile-filtered solution of TLR4 Inhibitor, TAK-242 (Cat. No. 614316) in DMSO.
重悬
Following initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 1 year at -70°C.
其他说明
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.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C15H17ClFNO4S |
分子量 | 361.82 |
产品性质
质量水平 | 100 |
测定 | ≥98% (HPLC) |
形式 | liquid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze avoid repeated freeze/thaw cycles desiccated (hygroscopic) protect from light |
储存温度 | −70℃ |
安全信息
储存分类代码 | 10 - Combustible liquids |
WGK | WGK 1 |
闪点(F) | 188.6 °F - (refers to pure substance) |
闪点(C) | 87 ℃ - (refers to pure substance) |