Overview
- Caseley, E.A. et al. (2016) Biochem. Pharmacol. 116, 130.
Alomone Labs ZINC9315614 inhibits human P2X7 receptors expressed in HEK-293 cells.Dose response curve of hP2X7 inhibition by ZINC9315614 (#Z-145). Cells were loaded with Fluo-8 NW dye, incubated with increasing concentrations of ZINC9315614, 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 355 nM.
- Caseley, E.A. et al. (2016) Biochem. Pharmacol. 116, 130.
- Stokes, L. et al. (2006) Br. J. Pharmacol. 149, 880.
ZINC9315614 is a selective antagonist of purinergic P2X7 receptors. It binds to the ATP-binding pocket of P2X71. ZINC9315614 inhibits YoPro1 dye uptake and BzATP-induced Ca2+ responses in HEK–human P2X7 cells with IC50 value of 0.8 µM and 3.2 µM, respectively1.
P2X receptors are cationic trimeric channel complexes that function as ATP-gated calcium-permeable and are considered to be an attractive therapeutic target. This family contains seven receptor subtypes: P2X1–P2X7. P2X7 receptors participate in various cellular responses such as membrane permeabilization, activation of caspases, cytokine release, cell proliferation, and apoptosis. P2X7 receptors can be found in almost all tissues1,2.
ZINC9315614 (#Z-145) is a highly pure, synthetic, and biologically active compound.
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