COA of Formula: C6H5NO2In 2022 ,《Synthesis and Evaluation of Novel 111In-Labeled Picolinic Acid-Based Radioligands Containing an Albumin Binder for Development of a Radiotheranostic Platform》 appeared in Molecular Pharmaceutics. The author of the article were Iikuni, Shimpei; Tarumizu, Yuta; Tsuchihashi, Shohei; Ohara, Takaki; Watanabe, Hiroyuki; Ono, Masahiro. The article conveys some information:
Picolinic acid-based metallic chelators, e.g., neunpa and octapa, have attracted much attention as promising scaffolds for radiotheranostic agents, particularly those containing larger α-emitting radiometals. Furthermore, albumin binder (ALB) moieties, which noncovalently bind to albumin, have been utilized to improve the pharmacokinetics of radioligands targeting various biomols. In this study, we designed and synthesized novel neunpa and octapa derivatives (Neunpa-2 and Octapa-2, resp.), which contained a prostate-specific membrane antigen (PSMA)-binding moiety (model targeting vector) and an ALB moiety. We evaluated the fundamental properties of these derivatives as radiotheranostic agents using 111In. In a cell-binding assay using LNCaP (PSMA-pos.) cells, [111In]In-Neunpa-2 and [111In]In-Octapa-2 specifically bound to the LNCaP cells. In addition, a human serum albumin (HSA)-binding assay revealed that [111In]In-Neunpa-2 and [111In]In-Octapa-2 exhibited greater binding to HSA than their non-ALB-conjugated counterparts ([111In]In-Neunpa-1 and [111In]In-Octapa-1, resp.). A biodistribution assay conducted in LNCaP tumor-bearing mice showed that the introduction of the ALB moiety into the 111In-labeled neunpa and octapa derivatives resulted in markedly enhanced tumor uptake and retention of the radioligands. Furthermore, single-photon emission computed tomog. imaging of LNCaP tumor-bearing mice with [111In]In-Octapa-2 produced tumor images. These results indicate that [111In]In-Octapa-2 may be a useful PSMA imaging probe and that picolinic acid-based ALB-conjugated radiometallic complexes may be promising candidates as radiotheranostic agents. In the experiment, the researchers used Picolinic acid(cas: 98-98-6COA of Formula: C6H5NO2)
Picolinic acid(cas: 98-98-6) is used as a chelate for alkaline earth metals. Used to prepare picolinato ligated transition metal complexes. In synthetic organic chemistry, has been used as a substrate in the Mitsunobu reaction and in the Hammick reaction.COA of Formula: C6H5NO2