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InSolution TLR4 Inhibitor, TAK-242-CAS 243984-11-4-Calbiochem
| 产品编号： | 4083555 |
| 规格： | A 25 mM (2 mg/221 μL) sterile-filtered solution of TLR4 Inhibitor, TAK-242 in DMSO. |
| CAS NO： | 243984-11-4 |
| 包装规格： | 2 MG |
| 产品类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
产品价格查看更多规格...
| 产品编号 | 包装单位 | 单价(元) | 国内现货 | 国外库存 | 询价单 |
| 4083555 | 2 MG | 1650 |
产品别名
243984-11-4
InSolution TLR4 Inhibitor, TAK-242-CAS 243984-11-4-Calbiochem
Ethyl-(6R)-6-(N-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-ene-1-carboxylate, (R)-Ethyl 6-(N-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-enecarboxylate, TLR4 Inhibitor, TAK-242 InSolution
TLR4 Inhibitor, TAK-242 InSolution, Ethyl-(6R)-6-(N-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-ene-1-carboxylate, (R)-Ethyl 6-(N-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-enecarboxylate
基本信息
| Empirical Formula【经验(实验)分子式】 | C15H17ClFNO4S |
| Molecular weight | 361.82 |
| General description【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.). |
| Biochem/physiol Actions【生化/生理作用】 | Cell permeable: yes Reversible: no Primary Target TLR4 |
| Warning【警告】 | Toxicity: Standard Handling (A) |
| Physical form【外形】 | A 25 mM (2 mg/221 µL) sterile-filtered solution of TLR4 Inhibitor, TAK-242 (Cat. No. 614316) in DMSO. |
| Reconstitution【重悬】 | Following initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 1 year at -70°C. |
| Other Notes【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. |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | liquid |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze avoid repeated freeze/thaw cycles desiccated (hygroscopic) protect from light |
| storage temp.【储存温度】 | −70℃ |
| packaging【包装】 | Packaged under inert gas |
安全信息
| Storage Class Code【储存分类代码】 | 10 - Combustible liquids |
| WGK | WGK 1 |
| Flash Point(F)【闪点(F)】 | 188.6 °F - (refers to pure substance) |
| Flash Point(C)【闪点(C)】 | 87 ℃ - (refers to pure substance) |
