GSK-5498A is a selective small molecule blocker of CRAC channel(IC50=1 uM); inhibit mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species.IC50 value: 1 uM [1]Target: CARC channel blocker GSK-5498A completely inhibited calcium influx through CRAC channels. This led to inhibition of the release of mast cell mediators and T-cell cytokines from multiple human and rat preparations. Mast cells from guinea-pig and mouse preparations were not inhibited by GSK-5498A.
[1]. Rice LV, et al. Characterization of selective Calcium-Release Activated Calcium channel blockers in mast cells and T-cells from human, rat, mouse and guinea-pig preparations. Eur J Pharmacol. 2013 Mar 15;704(1-3):49-57.