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AT791

CAS No. : 1219962-49-8

MCE 站：AT791

产品活性：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。

研究领域：Immunology/Inflammation

作用靶点：Toll-like Receptor (TLR)

In Vitro: 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) .
AT7916 suppresses TLR9-DNA interaction in vitro, with an IC₅₀ in the 1 to10 μM range.
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_as of 7.9 ａnd 6.1, ａnd E6446 has pK_as of 8.6 ａnd 6.5, indicating they would be more highly protonated in endolysosomal compartments compared with cytoplasm.

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

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