mouse p2x7 receptor

A-839977 is a selective P2X7 receptor antagonist with anti-inflammatory and analgesic properties, inhibiting BzATP-induced calcium efflux from the P2X7 receptor, and is used in the study of renal fibrosis.

AZ 11645373 (3-[1-[[(3'-NITRO[1,1'-BIPHENYL]-4-YL)OXY]METHYL]-3-(4-PYRIDINYL)PROPYL]-2,4-THIAZOLIDINEDIONE) is a highly selective and potent human P2X7 receptor antagonist that has no effect on mouse/rat P2X7 receptor.

JNJ-54166060 is a potent and selective P2X7 receptor antagonist, with IC50 values of 4 nM, 115 nM, and 72 nM for the human, rat, and mouse P2X7 receptors, respectively [1].

A-804598 is a competitive and selective P2X7 receptor antagonist (IC50: 10 nM, rat; 9 nM, mouse; 11 nM, human).

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)

Lu AF27139 is an effective and selective antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 can be used in CNS diseases studies.