GSK-5498A

• CAT Number: I001006
• CAS Number: 1253186-49-0
• Molecular Formula: C18H11F6N3O
• Molecular Weight: 399.29
• Purity: ≥95%
• Synonyms: 2,6-difluoro-N-[1-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]pyrazol-3-yl]benzamide
• InChI: InChI=1S/C18H11F6N3O/c19-12-4-1-3-11(18(22,23)24)10(12)9-27-8-7-15(26-27)25-17(28)16-13(20)5-2-6-14(16)21/h1-8H,9H2,(H,25,26,28)
• InChIKey: AUBGZAJDHUHMAE-UHFFFAOYSA-N
• SMILES: C1=CC(=C(C(=C1)F)CN2C=CC(=N2)NC(=O)C3=C(C=CC=C3F)F)C(F)(F)F

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].
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].

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.
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