Overview
- Caseley, E.A. et al. (2016) Biochem. Pharmacol. 116, 130.
Alomone Labs ZINC58368839 inhibits human P2X7 receptors expressed in HEK-293 cells.Dose response curve of hP2X7 inhibition by ZINC58368839 (#Z-135). Cells were loaded with Fluo-8 NW dye, incubated with increasing concentrations of ZINC58368839, 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 13 µM.
ZINC58368839 inhibits P2X7 receptors by binding to the ATP-binding pocket of the receptor and demonstrates strong specificity towards human P2X7R over human P2X4R and rat P2X3R1. It inhibits BzATP-induced Ca2+ responses in HEK–hP2X7 cells with IC50 value of 4.8 µM1.
P2X receptors are cationic trimeric channel complexes that function as ATP-gated Ca2+-permeable channels. They are considered to be an attractive therapeutic target. This family includes seven receptor subtypes: P2X1–P2X7. P2X7 receptors participate in a variety of cellular responses such as membrane permeabilization, activation of caspases, cytokine release, cell proliferation, and apoptosis. P2X7 receptors are ubiquitously expressed, and particularly in cells of haematopoietic origin1,2.
