3-o-Methylfluorescein phosphate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 英文名称: 3-o-Methylfluorescein phosphate
• 英文别名: 3-O-Methylfluorescein 6-phosphate；3-O-Methylfluoresceinphosphate；3-omethylfluorescein phosphate；OMFP；(6'-methoxy-3-oxospiro[2-benzofuran-1,9'-xanthene]-3'-yl) dihydrogen phosphate
• 化学式: C₂₁H₁₅O₈P
• 分子量: 426.319
• InChiKey: QWBZNOKUBXSLRE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  30
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  112
• 氢给体数：
  2
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  3-o-Methylfluorescein phosphate 、 MDF2085 在 human mitogen-activated protein kinase phosphatase-1 作用下， 反应 1.0h， 生成 3-O-methylfluorescein
  参考文献：
  名称：

  Structurally Unique Inhibitors of Human Mitogen-Activated Protein Kinase Phosphatase-1 Identified in a Pyrrole Carboxamide Library

  摘要：

  丝裂原活化蛋白激酶磷酸酶1（MKP-1）是一种酪氨酸磷酸酶超家族成员，能够去磷酸化并灭活重要的丝裂原活化蛋白激酶（MAPK）底物，如p38、c-Jun NH2末端激酶和细胞外信号调节激酶。尽管这些MAPK底物调控与人类疾病相关的许多基本细胞过程，但描述的药理学抑制剂寥寥无几。目前缺乏可获得的选择性MKP-1抑制剂严重限制了对MKP-1生物学角色的研究，这也是我们采用最近描述的三环吡咯-2-羧酰胺库进行筛选的一个理由。在本报告中，我们通过发现172个成员中有10个抑制了人类MKP-1，展示了吡咯羧酰胺库的药理学丰富性。其中两种吡咯羧酰胺，PSI2106和MDF2085，是重组人类MKP-1酶活性的显著体外抑制剂，IC50值分别为8.0 ± 0.9和8.3 ± 0.8 μM。两者对MKP-1的选择性优于密切相关的磷酸酶MKP-3、Cdc25B、VHR和PTP1B。计算分析催化位点附近的表面性质发现，所研究的磷酸酶在底物结合位点的静电势上存在显著差异。化合物对MKP-1的抑制是可逆的，但表现出混合动力学。在生理相关浓度的谷胱甘肽存在下，磷酸酶抑制得以保持。分子对接研究提示PSI2106可能与MKP-1上的His229和Phe299相互作用。这些结果显示了使用小型聚焦库识别药理学探针的效力。

  DOI：

  10.1124/jpet.107.122242

文献信息

• Dry analytical element for alkaline phosphatase assay
  申请人：EASTMAN KODAK COMPANY (a New Jersey corporation)

  公开号：EP0132830A2

  公开（公告）日：1985-02-13

  Disclosed herein is a dry analytical element and a method of using same for quantitatively detecting alkaline phosphatase in an aqueous liquid. The element comprises, in fluid contact, first and second reagent zones wherein the first reagent zone contains a substrate for alkaline phosphatase, e.g. p-nitrophenyl phosphate, and the second reagent zone contains a buffer which is an alkali metal or ammonium salt and has a pKa in the range of 9-11.5, e.g. an alkali metal salt of carbonic acid.

  本文公开了一种干式分析元件及其使用方法，用于定量检测水性液体中的碱性磷酸酶。该元件包括流体接触的第一试剂区和第二试剂区，其中第一试剂区含有碱性磷酸酶的底物，例如对硝基苯磷酸，第二试剂区含有缓冲液，缓冲液是碱金属盐或铵盐，pKa 在 9-11.5 之间，例如碳酸的碱金属盐。
• Integral multilayer analytical element for use in the measurement of alkaline phosphatase acitivity
  申请人：FUJI PHOTO FILM CO., LTD.

  公开号：EP0182179A1

  公开（公告）日：1986-05-28

  An integral multilayer analytical element for use in the measurement of alkaline phosphatase activity, which comprises a porous spreading layer of woven fabric or knitted fabric containing an alkaline phosphatase-sensitive self-developing substrate, a buffer layer containing one or more compounds functioning as a phosphoric acid acceptor and a buffering agent and a support layer in a laminated form.

  一种用于测量碱性磷酸酶活性的整体式多层分析元件，它包括多孔的机织物或针织物铺展层，其中含有对碱性磷酸酶敏感的自显影基质；缓冲层，其中含有一种或多种用作磷酸受体和缓冲剂的化合物；以及层压形式的支撑层。
• Integral multilayer analytical element for measurement of alkaline phosphatase activity
  申请人：FUJI PHOTO FILM CO., LTD.

  公开号：EP0205950A1

  公开（公告）日：1986-12-30

  An integral multilayer analytical element for the measurement of alkaline phosphatase activity, which comprises a porous spreading layer containing a self-developable substrate in response to contact with alkaline phosphatase, a buffer layer containing a diffusion-resistant base and a support in a laminated form.

  一种用于测量碱性磷酸酶活性的整体多层分析元件，它包括一个多孔铺展层，内含与碱性磷酸酶接触后可自动显影的基底；一个缓冲层，内含抗扩散基底；以及一个层叠形式的支撑物。
• Analytical element and method for theophylline determination having increased alkaline phosphatase isoenzyme
  申请人：EASTMAN KODAK COMPANY (a New Jersey corporation)

  公开号：EP0258035A2

  公开（公告）日：1988-03-02

  Theophylline can be determined with an analytical element and method which utilize the inhibition, by theophylline, of alkaline phosphatase activity on an appropriate substrate. The assay is carried out at a pH of 9 or less. The element contains a suitable buffer and first and second zones in fluid contact. The isoenzyme of alkaline phosphatase and a suitable substrate for the isoenzyme are located in different zones of the element. The isoenzyme is present in one of the zones in an amount of at least 100 I.U./m². This level of isoenzyme reduces or eliminates bias caused by endogenous alkaline phosphatase and hemoglobin during an assay.

  茶碱可以用一种分析元素和方法来测定，这种元素和方法利用茶碱对适当底物上碱性磷酸酶活性的抑制作用。检测在 pH 值为 9 或更低的条件下进行。检测元件包含合适的缓冲液以及液体接触的第一区和第二区。碱性磷酸酶同工酶和该同工酶的适当底物位于该元件的不同区域。其中一个区中的同工酶含量至少为 100 I.U./m²。这种水平的同工酶可减少或消除化验过程中内源性碱性磷酸酶和血红蛋白造成的偏差。
• Analytical element and method for theophylline determination using buffer in spreading zone
  申请人：EASTMAN KODAK COMPANY (a New Jersey corporation)

  公开号：EP0258034A2

  公开（公告）日：1988-03-02

  Theophylline can be determined with an analytical element and method which utilize the inhibition, by theophylline, of alkaline phosphatase activity on an appropriate substrate. The assay is carried out at a pH of 9 or less. The element comprises a porous spreading zone and at least one other zone in fluid contact with the spreading zone. The isoenzyme of alkaline phosphatase and a suitable substrate for the isoenzyme are located in different zones of the element. The element also contains a buffer for maintaining the pH at 9 or less, substantially all of which is located in the porous spreading zone.

  茶碱可以用一种分析元素和方法来测定，这种元素和方法利用茶碱对适当底物上碱性磷酸酶活性的抑制作用。检测在 pH 值为 9 或更低的条件下进行。检测元件包括一个多孔扩散区和至少一个与扩散区流体接触的其他区域。碱性磷酸酶同工酶和该同工酶的合适底物位于该元件的不同区域。该元件还含有用于将 pH 值保持在 9 或以下的缓冲剂，缓冲剂基本上全部位于多孔扩散区。