ith-15004

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-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)