| 产品描述: | 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 |
| 靶点: |
CRAC channel;Others |
| 体外研究: |
GSK-5498A (1 and 10 μM) inhibits calcium influx through CRAC channels in human embryonic kidney cells. 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. GSK-5498A (1 nM-10 μM) evokes concentration-dependent inhibition of Cytostim-evoked interferon-γ and IL-5 production in PBMCs. GSK-5498A (1 μM-10 μM) inhibits degranulation of rat tissue-resident mast cells. GSK-5498A (10 nM-10 μM) inhibits mouse and rat T-cell cytokine (IL-2) release. GSK-5498A (0-10 μM) shows high selectivity for CRAC channels over other ion channels, enzymes and G-protein coupled receptors |
| 参考文献: |
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. |
| 溶解性: |
soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.504 ml |
12.522 ml |
25.044 ml |
| 5 mM |
0.501 ml |
2.504 ml |
5.009 ml |
| 10 mM |
0.25 ml |
1.252 ml |
2.504 ml |
| 50 mM |
0.05 ml |
0.25 ml |
0.501 ml |
|
| 注意: |
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