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AT791 Sale

目录号 : GC62334

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。

AT791 Chemical Structure

Cas No.:1219962-49-8

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥2,970.00
现货
5 mg
¥2,700.00
现货
10 mg
¥4,320.00
现货
25 mg
¥8,550.00
现货
50 mg
¥13,050.00
现货
100 mg
¥20,250.00
现货

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Sample solution is provided at 25 µL, 10mM.

Description

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.

化学性质

Cas No. 1219962-49-8 SDF
分子式 C23H31N3O3 分子量 397.51
溶解度 DMSO : 25 mg/mL (62.89 mM; Need ultrasonic) 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

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1 mg 5 mg 10 mg
1 mM 2.5157 mL 12.5783 mL 25.1566 mL
5 mM 0.5031 mL 2.5157 mL 5.0313 mL
10 mM 0.2516 mL 1.2578 mL 2.5157 mL
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