ITH15004 is a non-nucleotide antagonist of the purinergic P2X7receptor (IC50= 9 µM in HEK293 cells expressing the human receptor).1It inhibits ATP-induced currents inX. laevisoocytes expressing the human P2X7receptor when used at a concentration of 100 µM. ITH15004 (1 µM) decreases IL-1beta release from LPS-primed, ATP-stimulated isolated mouse peritoneal macrophages. It has high permeability in a parallel artificial membrane permeability assay (PAMPA).
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