AT791
规格
| Cas Number | 1219962-49-8 |
| 规格或纯度 | ≥98% |
| 纯度 | ≥98% |
| 包装 | 100mg 或 50mg 或 10mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | DMSO : 100 mg/mL (251.57 mM; Need ultrasonic) |
| 过滤标签 | Toll-like Receptor (TLR),Immunology/Inflammation |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | AT791 是一种口服生物活性强的 TLR7 和 TLR9 抑制剂。AT791 可抑制多种人类和小鼠细胞类型中的 TLR7 和 9 信号传导，并可抑制 DNA 与 TLR9 在体外的相互作用。 |
| 英文描述 |
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 In Vitro 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). AT7916 suppresses TLR9-DNA interaction in vitro, with an IC 50 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 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:TLR7 3.33 μM (IC 50 ) TLR9 0.04 μM (IC 50 ) |