GSK-5498A
目录号: PL02742 纯度: ≥98%
CAS No. :1253186-49-0
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中文名称
GSK-5498A
中文别名
2,6-二氟-N-[1-[[2-氟-6-(三氟甲基)苯基]甲基]-1H-吡唑-3-基]苯甲酰胺
英文名称
GSK-5498A
英文别名
GSK-5498A;2,6-difluoro-N-[1-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]pyrazol-3-yl]benzamide;2,6-difluoro-N-(1-{[2-fluoro-6-(trifluoromethyl)phenyl]methyl}-1H-pyrazol-3-yl)benzamide;GSK5498A;GSK 5498A;BCP23928;GSK5498A;GSK 5498A;2,6-difluoro-N-{1-[2-fluoro-6-(trifluoromethyl)benzyl]-1H-pyrazol-3-yl}benzamide
Cas No.
1253186-49-0
分子式
C18H11F6N3O
分子量
399.29
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
GSK-5498A 是一种选择性的钙释放激活钙通道 (CARC channel) 抑制剂 (IC50: 1 μM). GSK-5498A 可抑制肥大细胞介质释放和 T 细胞促炎性细胞因子的释放。GSK-5498A 可用于炎症的研究。
生物活性
GSK-5498A is a selective CARC channel inhibitor (IC 50 : 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.
性状
Solid
IC50 & Target[1][2]
CRAC channel
体外研究(In Vitro)
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.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
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.
溶解度数据
In Vitro: DMSO : ≥ 100 mg/mL (250.44 mM)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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