AT791
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。
Cas No.:1219962-49-8
Sample solution is provided at 25 µL, 10mM.
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.
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 |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 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。 |
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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。 |
制备储备液 | |||
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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 |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet