Powder: -20°C for 3 years | In solvent: -80°C for 1 year
E6446 dihydrochloride 是一种新型合成拮抗剂,用于核酸感应 TLR;有效抑制对 HEK:TLR9 细胞的 DNA 刺激,IC50 为 10 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,160 | 现货 | ||
2 mg | ¥ 1,720 | 现货 | ||
5 mg | ¥ 2,530 | 现货 | ||
10 mg | ¥ 3,730 | 现货 | ||
25 mg | ¥ 5,970 | 现货 | ||
50 mg | ¥ 7,880 | 现货 | ||
100 mg | ¥ 10,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 3,130 | 现货 |
产品描述 | E6446 dihydrochloride is a novel synthetic antagonist for nucleic acid-sensing TLRs; potently suppressed DNA stimulation of HEK:TLR9 cells with IC50 of 10 nM. |
靶点活性 | TLR9:10 nM. |
体外活性 | E6446 potently inhibited IL-6 production induced by CpG2216 but was ineffective against induction by the TLR3 ligand poly inosine-cytosine. E6446 showed a modest but consistent superiority over AT791, and both were significantly more potent than hydroxychloroquine. Significantly, 250 nM and 1.25 μM E6446 completely suppressed all of the CpG oligo-induced changes in gene expression [1]. E6446 specifically inhibited TLR9 activation with CpG ODN 2006, in the range of 0.01–0.03 μM. A 100-fold higher concentration (2–8 μM) of E6446 was required to inhibit TLR7/8 activated by the imidazoquinoline compound R848 [2]. |
体内活性 | To test their activity in vivo, mice were orally dosed with 20 mg/kg of AT791 or E6446 and 18 hours later were challenged with 60 μg CpG1668 oligonucleotide injected subcutaneously. CpG1668-induced IL-6 production was inhibited ~50% by AT791 and almost completely by E6446 [1]. therapy with E6446 diminished the activation of TLR9 and prevented the exacerbated cytokine response observed during acute Plasmodium infection [2]. |
分子量 | 522.51 |
分子式 | C27H37Cl2N3O3 |
CAS No. | 1345675-25-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 5.22 mg/mL (10 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9138 mL | 9.5692 mL | 19.1384 mL | 47.846 mL |
5 mM | 0.3828 mL | 1.9138 mL | 3.8277 mL | 9.5692 mL | |
10 mM | 0.1914 mL | 0.9569 mL | 1.9138 mL | 4.7846 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
E6446 dihydrochloride 1345675-25-3 Immunology/Inflammation TLR E-6446 Dihydrochloride E-6446 E 6446 Dihydrochloride E6446 E-6446 dihydrochloride E 6446 E6446 Dihydrochloride Inhibitor inhibitor inhibit