ITH15004 is a non-nucleotide antagonist of the purinergic P2X7 receptor (IC50 = 9 µM in HEK293 cells expressing the human receptor).1 It inhibits ATP-induced currents in X. laevis oocytes expressing the human P2X7 receptor when used at a concentration of 100 µM. ITH15004 (1 µM) decreases IL-1β release from LPS-primed, ATP-stimulated isolated mouse peritoneal macrophages. It has high permeability in a parallel artificial membrane permeability assay (PAMPA).
1.Calzaferri, F., Narros-FernÁndez, P., de Pascual, R., et al.Synthesis and pharmacological evaluation of novel non-nucleotide purine derivatives as P2X7 antagonists for the treatment of neuroinflammationJ. Med. Chem.64(4)2272-2290(2021)