| Bioactivity | GSK-5498A is a selective CARC channel inhibitor (IC50: 1 μM). GSK-5498A inhibits mediators release from mast cells and pro-inflammatory cytokines release from T cells. GSK-5498A can be used in the research of inflammatory disorders[1]. | ||||||||||||
| Target | CRAC channel | ||||||||||||
| Invitro | GSK-5498A (1 and 10 μM) inhibits calcium influx through CRAC channels in human embryonic kidney cells[1].GSK-5498A (1 nM-10 μM) inhibits the thapsigargin-evoked fluorescence signal (pIC50: 6.3) in Jurkat cells, measured using the calcium sensitive dye: Fluo4-AM[1].GSK-5498A (1 nM-10 μM) evokes concentration-dependent inhibition of Cytostim-evoked interferon-γ and IL-5 production in PBMCs[1].GSK-5498A (1 μM-10 μM) inhibits degranulation of rat tissue-resident mast cells[1].GSK-5498A (10 nM-10 μM) inhibits mouse and rat T-cell cytokine (IL-2) release[1].GSK-5498A (0-10 μM) shows high selectivity for CRAC channels over other ion channels, enzymes and G-protein coupled receptors[1]. | ||||||||||||
| Name | GSK-5498A | ||||||||||||
| CAS | 1253186-49-0 | ||||||||||||
| Formula | C18H11F6N3O | ||||||||||||
| Molar Mass | 399.29 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |