产品说明书
GSK-7975A
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同义名 : | - |
| CAS号 : | 1253186-56-9 | |
| 货号 : | A724629 | |
| 分子式 : | C18H12F5N3O2 | |
| 纯度 : | 98% | |
| 分子量 : | 397.299 | |
| MDL号 : | MFCD28411366 | |
| 存储条件： |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 95 mg/mL(239.11 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The Ca2+ current passing through the plasma membrane is known as the Ca2+ release-activated Ca2+ (CRAC) current, and it is believed to play a central role in many physiological processes such as gene transcription, proliferation, and cytokine release. GSK-7975A is a potent and orally available CRAC channel blocker with an IC50 of 0.34 μM. GSK-7975A (1 μM) reduced FcεRI-dependent Ca2+ influx and 3 μM of it reduced the release of histamine, leukotriene C4, and cytokines (IL-5/-8/-13 and TNFα) by up to 50%[4]. GSK-7975A separately inhibited toxin-induced activation of ORAI1 and/or activation of Ca2+ currents after Ca2+ release, in a concentration-dependent manner, in mouse and human pancreatic acinar cells. In 3 clinically representative mouse models of acute pancreatitis, GSK-7975A inhibited all local and systemic features of acute pancreatitis in all 3 models, in dose- and time-dependent manners[5]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.52mL 0.50mL 0.25mL |
12.58mL 2.52mL 1.26mL |
25.17mL 5.03mL 2.52mL |
| 参考文献 |
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