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S89346

RU.521

源叶(MedMol) 98%
  • 英文名:
  • 3-(1-(6,7-Dichloro-1H-benzo[d]imidazol-2-yl)-5-hydroxy-3-methyl-1H-pyrazol-4-yl)isobenzofuran-1(3H)-one
  • 别名:
  • RU320521;3-(1-(6,7-二氯-1H-苯并[d]咪唑-2-基)-5-羟基-3-甲基-1H-吡唑-4-基)异苯并呋喃-1(3H)-酮
  • CAS号:
  • 2262452-06-0
  • 分子式:
  • C19H12Cl2N4O3
  • 分子量:
  • 415.23
  • 核磁/质谱:
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S89346-5mg 98% ¥580.00元 2 - - - EA 加入购物车
源叶(MedMol) S89346-10mg 98% ¥870.00元 1 - - - EA 加入购物车
源叶(MedMol) S89346-25mg 98% ¥1400.00元 2 - - - EA 加入购物车
源叶(MedMol) S89346-100mg 98% ¥4300.00元 4 - - - EA 加入购物车
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产品介绍

参考文献(1篇)

质检证书(COA)

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  • 产品描述: RU.521 (RU320521) is a potent dsDNA inhibitor (IC50 : 700 nM), inhibition of the dsDNA pathway by RU.521 requires the presence of cGAS.
  • 靶点: DNA; cGAS;DNA; cGAS
  • 体内研究:
    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 16h prior in 96-well dishes, then harvested 72h 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.
  • 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.
  • 溶解性: Soluble  in  DMSO
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.408 ml 12.042 ml 24.083 ml
    5 mM 0.482 ml 2.408 ml 4.817 ml
    10 mM 0.241 ml 1.204 ml 2.408 ml
    50 mM 0.048 ml 0.241 ml 0.482 ml
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