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E6446 dihydrochloride

CAS号

1345675-25-3

分子式

C27H37Cl2N3O3

主要靶点

TLR

仅限科研使用

Cat No : CM06666

Print datasheet

Synonyms

E 6446|E 6446 Dihydrochloride|E6446|E-6446|E6446 dihydrochloride|E6446 Dihydrochloride|E-6446 Dihydrochloride|E-6446 dihydrochloride|TLR

验证数据展示

  • CAS No.: 1345675-25-3

    E6446 dihydrochloride
    CAS#: 1345675-25-3

产品信息

CAS号 1345675-25-3
分子式 C27H37Cl2N3O3
主要靶点 TLR
主要通路 免疫与炎症
分子量 522.51
纯度 99.44%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 E 6446|E 6446 Dihydrochloride|E6446|E-6446|E6446 dihydrochloride|E6446 Dihydrochloride|E-6446 Dihydrochloride|E-6446 dihydrochloride|TLR

靶点活性

TLR9:10 nM.

体内活性

为了测试其体内活性，小鼠通过口服方式给予AT791或E6446，剂量为20 mg/kg，18小时后，通过皮下注射60 μg CpG1668寡核苷酸进行挑战。CpG1668诱导的IL-6产生被AT791抑制约50%，而E6446几乎完全抑制了IL-6产生[1]。E6446治疗降低了TLR9的激活，并阻止了在急性恶性疟疾感染期间观察到的细胞因子反应的加剧[2]。

体外活性

E6446有效地抑制了由CpG2216引起的IL-6产生，但对TLR3配体poly inosine-cytosine的激活无效。在与AT791比较中，E6446表现出适度但一致的优势，且两者均显著优于羟氯喹。值得注意的是，250 nM和1.25 μM的E6446完全抑制了CpG寡核苷酸引起的所有基因表达变化[1]。E6446在0.01–0.03 μM范围内特异性抑制TLR9与CpG ODN 2006的活化。抑制通过imidazoquinoline化合物R848激活的TLR7/8，需要E6446浓度高达2–8 μM，是前者的100倍[2]。

溶解度

DMSO:5.22 mg/mL (10 mM)

参考文献

1.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.
2.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.

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