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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。
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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 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 396 | 现货 | |
2 mg | ¥ 585 | 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 | ¥ 7,260 | 现货 | |
200 mg | ¥ 9,790 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 889 | 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 | 将初代BMDMs处理RU.521或其类似物,可减少小鼠IFNB1表达,表明它们在抑制缺乏细胞质DNA外切酶的细胞中固有的、构成性激活的I型干扰素表达方面的有效性。 |
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 |
Smiles | Cc1nn(c(O)c1C1OC(=O)c2ccccc12)-c1nc2ccc(Cl)c(Cl)c2[nH]1 |
密度 | 1.73 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 125 mg/mL (301.04 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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