| 产品描述： | E6446 inhibits Toll-like receptor (TLR)7 and 9 signaling. E6446 works in a variety of human and mouse cell types and inhibits DNA-TLR9 interaction in vitro. When administered to mice, this compound suppress responses to challenge doses of cytidine-phosphate-guanidine (CpG)-containing DNA, which stimulates TLR9 |
| 靶点： |
TLR |
| 体外研究： |
Measurement of ELAM-1–luciferase activity showed that E6446 specifically inhibited TLR9 activation with CpG ODN 2006, in the range of 0.01–0.03 μM. A 100-fold higher concentration (2–8 μM) of E6446 was required to inhibit TLR7/8 activated by the imidazoquinoline compound R848. Incubation of cells with even higher concentrations (30 μM) of E6446 was required to reduce 50% of TLR4 activation (Fig. 2A). Reference: Proc Natl Acad Sci U S A. 2011 Mar 1; 108(9): 3689–3694. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3048158/ |
| 体内研究： |
E6446 treatment significantly reduced LV chamber size and improved cardiac function in TAC-operated mice. Reference: JACC Basic Transl Sci. 2019 Jun; 4(3): 348–363. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6610159/ |
| 参考文献： |
1. Franklin BS, et al. Therapeutical targeting of nucleic acid-sensing Toll-like receptors prevents experimental cerebral malaria. Proc Natl Acad Sci U S A. 2011 Mar 1;108(9):3689-94. 2. Lamphier M, et al. Novel small molecule inhibitors of TLR7 and TLR9: mechanism of action and efficacy in vivo. Mol Pharmacol. 2014 Mar;85(3):429-40. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.224 ml |
11.121 ml |
22.242 ml |
| 5 mM |
0.445 ml |
2.224 ml |
4.448 ml |
| 10 mM |
0.222 ml |
1.112 ml |
2.224 ml |
| 50 mM |
0.044 ml |
0.222 ml |
0.445 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京