货号：T5947
储存条件：粉末-20°C可保存3年；液体-80°C可保存12月。
产品描述
TAK-242 is a novel TLR4 (Toll-like receptor 4) inhibitor with IC50 values of 1.1-33nM for inhibition of LPS-induced production of NO, TNF-α and IL-6 in RAW264.7 cells, mouse peritoneal macrophages and PBMCs. TAK-242 inhibited both MyD88-independent and -dependent pathway, independent of LPS concentration and types of TLR4 ligands. It did not affect LPS-induced conformational change of TLR4-MD-2 and TLR4 homodimerization. A 60-μg dose of TAK-242 to neonatal CCM (cerebral cavernous malformations) disease model (susceptible Krit1ECKO mice) reduced CCM lesion volume by 80%. Intravenous administration of TAK-242 at dose of 1mg/kg and 3mg/kg 1 h before LPS challenge could protect mice from LPS-induced lethality.
产品信息
CAS号 | 243984-11-4 | |
分子式 | C15H17ClFNO4S | |
分子量 | 361.82 | |
溶解度 | DMSO | 140.0 mg/mL (386.9 mM) |
储存液制备
储存液制备 | 1 mg | 5 mg | 10 mg | |
1 mM | 2.7638 mL
| 13.8190 mL
| 27.6381 mL
| |
5 mM | 0.5528 mL
| 2.7638 mL
| 5.5276 mL
| |
10 mM | 0.2764 mL
| 1.3819 mL
| 2.7638 mL
|
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