| 1426251-47-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• CAS: 1426251-47-9
• 化学式: C₁₅H₂₆N₄O₄
• 分子量: 326.396
• InChiKey: ILZVGQGJFUTKBZ-UHFFFAOYSA-N

反应信息

• 作为反应物：
  描述：

  在 水 、 potassium carbonate 、 potassium iodide 、 sodium hydroxide 作用下， 以 四氢呋喃 、 乙腈 为溶剂， 反应 18.0h， 生成 1-(2-((2-(tert-butoxycarbonylamino)ethyl)(3-carboxypropyl)amino)ethyl)-1H-pyrazole-4-carboxylic acid
  参考文献：
  名称：

  Influence of the Bifunctional Chelator on the Pharmacokinetic Properties of ^99mTc(CO)₃-Labeled Cyclic α-Melanocyte Stimulating Hormone Analog

  摘要：

  Aiming at the design of specific melanocortin-1 receptor (MC1R) targeted imaging probes, we report on the effect of different azolyl-ring substitution patterns (carboxylate at the 4-position and/or methyl groups at the 3,5 positions) of pyrazolyldiamine bifunctional chelators (Pz(2)-Pz(4)) on the pharmacokinetic profile of the Tc-99m(CO)(3)-labeled lactam bridge-cyclized alpha-melanocyte stimulating hormone derivative, beta AlaNleCycMSH(hex). Three pyrazolyl-diamine-containing chelators were conjugated to beta AlaNleCycMSH(hex), with the resulting peptide conjugates displaying subnanomolar MC1R binding affinity. Biodistribution studies in B16F1 melanoma-bearing mice show that all radiopeptides present a good melanoma uptake. The introduction of a carboxylate group in the azolyl-ring leads to a remarkable reduction of the kidney (>89%) and liver (>91%) accumulation for Tc-99m(CO)(3)-Pz(3)-beta AlaNleCycMSH(hex) and Tc-99m(CO)(3)-Pz(4)-beta AlaNleCycMSH(hex) when compared to the radiopeptide Tc-99m(CO)(3)-Pz(1)-beta AlaNleCycMSH(hex), where that group is absent. The good tumor uptake and favorable tumor-to-nontarget-organs ratios of Tc-99m(CO)(3)-Pz(3)-beta AlaNleCycMSH(hex) and Tc-99m(CO)(3)-Pz(4)-beta AlaNleCycMSH(hex) highlights the potential of both compounds as melanoma imaging agents.

  DOI：

  10.1021/jm301647t