- Alomone Labs AZ 10606120 dihydrochloride inhibits human P2X7 receptors expressed in HEK-293 cells.Dose-response curve of hP2X7 inhibition by AZ 10606120 dihydrochloride (#A-405). Cells were loaded with Fluo-8 NW dye, incubated with increasing concentrations of AZ 10606120 dihydrochloride, 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 8.15 nM.
AZ 10606120 dihydrochloride is a potent and selective noncompetitive antagonist of the P2X7 receptor with IC50 value of ~10 nM2. The compound shows little or no effect at other P2X receptor subtypes1,2. In studies conducted in animal models, AZ 10606120 treatment shows antidepressant effects and reduces tumor growth2.
P2X receptors are a family of ligand-gated cation channels activated by the binding of extracellular ATP. Seven members of this family have been identified and function in homomeric or heteromeric combinations. P2X7 receptor is a therapeutic target due to its potential involvement in pain and inflammatory disorders1,2.
AZ 10606120 dihydrochloride (#A-405) is a highly pure, synthetic, and biologically active compound.