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

半岛bd体育手机客户端 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 micein vivo. Complete elimination of septic shock-induced death can be extended to liveE. 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 ?L) 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

半岛bd体育手机客户端 性质

安全信息