Parallel fluorescent probe synthesis based on the large-scale preparation of BODIPY FL propionic acid |
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Authors: | Taisuke Katoh Masato Yoshikawa Takeshi Yamamoto Ryosuke Arai Noriyuki Nii Yoshihide Tomata Shinkichi Suzuki Ryoukichi Koyama Nobuyuki Negoro Takatoshi Yogo |
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Institution: | Pharmaceutical Research Division, Takeda Pharmaceutical Company, Ltd., 26-1, Muraokahigashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan |
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Abstract: | We describe a methodology for quick development of fluorescent probes with the desired potency for the target of interest by using a method of parallel synthesis, termed as Parallel Fluorescent Probe Synthesis (Parallel-FPS). BODIPY FL propionic acid 1 is a widely used fluorophore, but it is difficult to prepare a large amount of 1, which hinders its use in parallel synthesis. Optimization of a synthetic scheme enabled us to obtain 50 g of 1 in one batch. With this large quantity of 1 in hand, we performed Parallel-FPS of BODIPY FL-labeled ligands for estrogen related receptor-α (ERRα). An initial trial of the parallel synthesis with various linkers provided a potent ligand for ERRα (Reporter IC50 = 80 nM), demonstrating the usefulness of Parallel-FPS. |
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Keywords: | BODIPY FL propionic acid Bulk preparation Parallel fluorescent probe synthesis ERRα |
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