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AT791
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AT791图片
规格:98%
分子量:397.51
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
AT791 是一种有效的口服生物利用 TLR7 和 TLR9 抑制剂。AT791 抑制多种人类和小鼠细胞类型的 TLR7 和 TLR9 信号传导,并在体外抑制 DNA-TLR9 相互作用。
货号:ajcx33516
CAS:1219962-49-8
分子式:C23H31N3O3
分子量:397.51
溶解度:DMSO : 25 mg/mL (62.89 mM; Need ultrasonic)
纯度:98%
存储:Store at -20°C
库存:现货

Background:

AT791 is a potent and orally bioavailable TLR7 and TLR9 inhibitor. AT791 inhibits TLR7 and 9 signaling in a variety of human and mouse cell types and inhibits DNA-TLR9 interaction in vitro[1].

AT791 potently suppresses DNA stimulation of HEK:TLR9 cells, with IC50 of 0.04 μM and is significantly less effective at suppressing R848 stimulation of HEK:TLR7 cells (IC50= 3.33 μM) [1].AT7916 suppresses TLR9-DNA interaction in vitro, with an IC50 in the 1 to10 μM range[1].AT791 and E6446 are typical of "lysosomotropic"compounds in that they are lipophilic and contain weak base amines. At neutral pH, such compounds are nonpolar and can penetrate lipid membranes, but within low pH vesicles they become protonated and are trapped (de Duve et al., 1974). Capillary electrophoresis showed that AT791 has pKas of 7.9 and 6.1, and E6446 has pKas of 8.6 and 6.5, indicating they would be more highly protonated in endolysosomal compartments compared with cytoplasm[1].

Short-term induction of serum interleukin-6 in mice by CpG1668 DNA is effectively suppresses by pretreatment with AT791 (20 mg/kg; p.o.)[1].

[1]. Lamphier M, et al. Novel small molecule inhibitors of TLR7 and TLR9: mechanism of action and efficacy in vivo. Mol Pharmacol. 2014;85(3):429-440.