S89473 |
E6446 |
源叶(MedMol) | 98% |
- 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: -20℃
- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)