TAC-Lime | 934488-77-4

• 英文名称: TAC-Lime
• CAS: 934488-77-4
• 化学式: C₆₀H₈₀BF₂N₅O₁₂
• 分子量: 1112.13
• InChiKey: QBGSLWYDMWWVHW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  None
• 重原子数：
  None
• 可旋转键数：
  None
• 环数：
  None
• sp3杂化的碳原子比例：
  None
• 拓扑面积：
  None
• 氢给体数：
  None
• 氢受体数：
  None

反应信息

• 作为反应物：
  描述：

  TAC-Lime 在 sodium hydroxide 作用下， 以 乙醇 、 水 为溶剂， 反应 2.0h， 生成
  参考文献：
  名称：

  Cell-Based Fluorescence Screen for K⁺ Channels and Transporters Using an Extracellular Triazacryptand-Based K⁺ Sensor

  摘要：

  K, channels and K(+)-coupled membrane transporters are important targets for drug discovery. We previously developed a triazacryptand (TAG)-based K(+) sensor, TAG-Red, and demonstrated its utility to image K(+) waves in mouse brain in vivo (Padmawar et al. Nat. Methods. 2005, 2, 825-827). Here, we synthesized a green-fluorescing dextran conjugate of TAC-bodipy ("TAC-Lime(dax)") for use as an extracellular K(+) sensor and demonstrated its utility in measuring K(+) transport across cell membranes. TAC-Lime(dex) fluorescence increased by 50% with increasing [K(+)] from 0 to 2 mM and was insensitive to [Na(+)], [Cl(-)], or pH. K(+) efflux from cells was quantified from increasing extracellular TAC-Limedex fluorescence following cell immersion in K(+)-free buffer. In HT-29 cells, K(+) efflux was 2.0 +/- 0.1 mu mol/cm(2)/s, increasing 8-fold following K(+) channel activation by ATP: the increase in K(+) efflux was inhibited by a K(+) channel blocker or by preventing cytoplasmic calcium elevation. Electroneutral K(+)/Cl(-) cotransport was demonstrated in SiHa cells, in which K(+) efflux was increased 3-fold by hypotonic challenge, the increase in K(+) efflux was fully inhibited by a K(+)/Cl(-) transport blocker. K(+) efflux measurements were adapted to a commercial fluorescence platereader for automated screening. The fluorescence-based K(+) transport assay largely replaces assays requiring radioactive rubidium and is suitable for high-throughput identification of K(+) transport modulators.

  DOI：

  10.1021/ja8014499
• 作为产物：
  描述：

  在 N,N-二异丙基乙胺 、 三氟化硼乙醚 作用下， 以 二氯甲烷 为溶剂， 反应 2.0h， 生成 TAC-Lime
  参考文献：
  名称：

  WO2007/44866

  摘要：

  公开号：