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InSolution TLR4 Inhibitor, TAK-242-CAS 243984-11-4-Calbiochem

品牌
Sigma-Aldrich
CAS
243984-11-4
货号
5.08336
规格纯度
A 25 mM (2 mg/221 μL) sterile-filtered solution of TLR4 Inhibitor, TAK-242 in DMSO.
参考价格
1504.15 *本价格含增值税费
促销
数量
-+
产品介绍:

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/tradenameCalbiochem®
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
WGKWGK 1
闪点(F)188.6 °F - (refers to pure substance)
闪点(C)87 ℃ - (refers to pure substance)

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