Every lot is tried & tested in a relevant biological assay.
- Swanson, D.M. et al. (2016) J. Med. Chem. 59, 8535.
- Alomone Labs JNJ-54166060 inhibits human P2X7 receptors expressed in HEK-293 cells.Dose response curve of hP2X7 inhibition by JNJ-54166060 (#J-125). Cells were loaded with Fluo-8 NW dye, incubated with increasing concentrations of JNJ-54166060, and stimulated with 80 µM BzATP. Changes in intracellular Ca2+ following agonist application were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™. IC50 was calculated at 65.6 nM.
JNJ-54166060 is a potent and selective antagonist of P2X7 receptors, displaying IC50 values of 4 nM for human P2X71. JNJ-54166060 has a high oral bioavailability with low-moderate clearance in preclinical species, and acceptable safety margins in rats1.
P2X receptors are a family of ion channels gated by ATP, a ubiquitous energy donor and receptor ligand in living cells. P2X receptors are ubiquitously expressed, including expression in neuronal, muscular, epithelial and immune cells and play a pivotal role in models of various pain conditions. P2X7 is responsible for mediating the release of proinflammatory cytokines known to have roles in inflammatory/immune conditions and pain2,3.