RU.521 (Synonyms: RU320521)
目录号: PL02180 纯度: ≥99%
CAS No. :2262452-06-0
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中文名称
RU.521
英文名称
RU.521
英文别名
RU.521;2-(4,5-Dichloro-1H-benzimidazol-2-yl)-5-methyl-4-(3-oxo-1H-2-benzofuran-1-yl)-1H-pyrazol-3-one
Cas No.
2262452-06-0
分子式
C19H12Cl2N4O3
分子量
415.23
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
RU.521 (RU320521) 是一种有效的,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。RU.521 也抑制 dsDNA 报告基因的活性,IC50 为 0.7 μM。RU.521 可以降低来自 Aicardi-Goutières 综合征小鼠模型的巨噬细胞中干扰素的组成型表达。
生物活性
RU.521 (RU320521) is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor and inhibits cGAS-mediated interferon upregulation. RU.521 suppresses dsDNA-activated reporter activity with an IC 50 of 0.7 μM. RU.521 reduces constitutive expression of interferon in macrophages from a mouse model of Aicardi-Goutières syndrome (AGS).
性状
Solid
IC50 & Target[1][2]
IC50: 0.7 μM (dsDNA)
体外研究(In Vitro)
RU.521 (0.1 nM-1000 μM; 72 h) suppresses dsDNA-induced signaling in macrophage cells.
RU.521(0-100 μM; 24 h) selectively inhibits cGAS-mediated signaling. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
RU.521 (5 mg/kg ; i.p. once) reduces symptoms from sepsis in mice. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male 8-week-old male mice with LPS injection
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Vincent J, et al. Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice. Nat Commun. 2017 Sep 29;8(1):750.
[2]. Xu Q, et al. Small molecule inhibition of cyclic GMP-AMP synthase ameliorates sepsis-induced cardiac dysfunction in mice. Life Sci. 2020 Nov 1;260:118315.
溶解度数据
In Vitro: DMSO : 83.33 mg/mL (200.68 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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