Characterization of the Active Enantiomer and Mapping of the Stereospecific Intermolecular Pattern of a Reference P2X7 Allosteric Antagonist.

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Tác giả: Kiera Bailey, Amélie Barczyk, Luciano Barluzzi, Simon J Coles, Xavier Dezitter, Lewis Edmunds, Barnaby W Greenland, Daniel Guest, David Leach, Andrew McGown, Régis Millet, Jordan Nafie, Nicolas Renault, John Spencer, Léa Sutton, Graham J Tizzard, Daniel von Emloh

Ngôn ngữ: eng

Ký hiệu phân loại:

Thông tin xuất bản: United States : ACS pharmacology & translational science , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 470568

The P2X purinergic receptor 7 (P2X7) has an essential role in inflammation, innate immunity, tumor progression, neurodegenerative diseases, and several other diseases, leading subsequently to the development of P2X7 modulators. AZ11645373 is a frequently studied P2X7 antagonist tool compound but always used as a racemic mixture. Racemic AZ11645373 can be separated into its respective enantiomers by chiral chromatography, albeit in small batches, and these were stereochemically intact over two years later, by chiral high-performance liquid chromatography (HPLC) analysis. On a higher scale, significant decomposition is observed during purification. One of the enantiomers was crystallized as a palladium complex, and its (
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