Powder: -20°C for 3 years | In solvent: -80°C for 1 year
RU.521 (RU3205217) 是选择性的环状 GMP-AMP 合成酶 (cGAS) 抑制剂,抑制 cGAS 介导的干扰素上调。它也抑制dsDNA 激活受体的活性,IC50为 700 nM。它可降低来自 Aicardi-Goutières 综合征小鼠模型的巨噬细胞中干扰素的组成型表达。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 413 | 现货 | ||
2 mg | ¥ 598 | 现货 | ||
5 mg | ¥ 970 | 现货 | ||
10 mg | ¥ 1,730 | 现货 | ||
25 mg | ¥ 3,590 | 现货 | ||
50 mg | ¥ 5,190 | 现货 | ||
100 mg | ¥ 7,350 | 现货 | ||
500 mg | ¥ 14,700 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 980 | 现货 |
产品描述 | RU.521 (RU3205217) is a potent dsDNA inhibitor (IC50 : 700 nM), inhibition of the dsDNA pathway by RU.521 requires the presence of cGAS. |
靶点活性 | dsDNA:700 nM |
体内活性 | Treatment of primary BMDMs with RU.521 or its analogs reduced IFNB1 expression in mice, indicating their effectiveness in suppressing intrinsic DNA-dependent, constitutively-activated type I interferon expression in cells deficient of a cytoplasmic DNA exonuclease. |
细胞实验 | Small-molecule compounds were serially diluted to concentrations spanning the range tested in the response curves were added to 6.7?×?10^5 RAW-Blue macrophages plated 16?h prior in 96-well dishes, then harvested 72?h after compound addition. ATP was measured using CellTiter Glo Viability Assay using 50?μM Tamoxifen as a positive control for cytotoxicity. Viability values were generated using vehicle (DMSO) or the first dose as 100% and Tamoxifen as 0%. Outliers were removed. |
动物实验 | the chronically elevated levels of cytokines observed in Trex1 null mice are a consequence of constitutively activated cGAS, due to the inability to eliminate aberrantly localized self-DNA. We harvested BMDMs from 6–8-week old Trex1 ?/? mice, treated them with each compound, and measured expression levels of IFNB1 by quantitative reverse transcription PCR (qRT-PCR). Treatment of primary BMDMs with RU.521 or its analogs reduced IFNB1 expression, indicating their effectiveness in suppressing intrinsic DNA-dependent, constitutively-activated type I interferon expression in cells deficient of a cytoplasmic DNA exonuclease. |
别名 | RU320521 |
分子量 | 415.23 |
分子式 | C19H12Cl2N4O3 |
CAS No. | 2262452-06-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL (301.04 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4083 mL | 12.0415 mL | 24.083 mL | 60.2076 mL |
5 mM | 0.4817 mL | 2.4083 mL | 4.8166 mL | 12.0415 mL | |
10 mM | 0.2408 mL | 1.2042 mL | 2.4083 mL | 6.0208 mL | |
20 mM | 0.1204 mL | 0.6021 mL | 1.2042 mL | 3.0104 mL | |
50 mM | 0.0482 mL | 0.2408 mL | 0.4817 mL | 1.2042 mL | |
100 mM | 0.0241 mL | 0.1204 mL | 0.2408 mL | 0.6021 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。
RU.521 2262452-06-0 DNA Damage/DNA Repair Immunology/Inflammation DNA cGAS inflammatory oxidative stress Inhibitor inhibit RU 320521 Cyclic GMP-AMP Synthase RU-320521 RU320521 signaling pathway inhibitor