化合物 AT791 T61882

Product Introduction
Bioactivity


英文名: AT791

描述: AT791 是一种有效的，具有口服活性的 TLR7和 TLR9抑制剂。AT791 对多种类型人类和小鼠细胞中的 TLR7 和 TLR9 信号传导具有抑制作用。AT791在体外抑制 DNA-TLR9 相互作用。

体外活性: AT791 potently suppresses DNA stimulation of HEK:TLR9 cells, with IC 50 of 0.04 μM and is significantly less effective at suppressing R848 stimulation of HEK:TLR7 cells (IC 50 = 3.33 μM) [1]. AT7916 suppresses TLR9-DNA interaction in vitro, with an IC 50 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 pK a s of 7.9 and 6.1, and E6446 has pK a s of 8.6 and 6.5, indicating they would be more highly protonated in endolysosomal compartments compared with cytoplasm [1].

体内活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途