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首页 / 抑制剂/激动剂 / 膜转运蛋白 / CRAC通道 / GSK-7975A

GSK-7975A {[allProObj[0].p_purity_real_show]}

货号：A724629

GSK-7975A is a potent and orally available CRAC channel inhibitor.

GSK-7975A 化学结构 CAS号：1253186-56-9
GSK-7975A 化学结构
CAS号：1253186-56-9
GSK-7975A 3D分子结构
CAS号：1253186-56-9
GSK-7975A 化学结构 CAS号：1253186-56-9
GSK-7975A 3D分子结构 CAS号：1253186-56-9
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GSK-7975A 纯度/质量文件 产品仅供科研

货号：A724629 标准纯度： {[allProObj[0].p_purity_real_show]}
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GSK-7975A 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].

GSK-7975A 参考文献

[1]Ashmole I, et al. CRACM/Orai ion channel expression and function in human lung mast cells. J Allergy Clin Immunol. 2012 Jun;129(6):1628-35.e2.

[2]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.

[3]Wen L, et al. Inhibitors of ORAI1 Prevent Cytosolic Calcium-Associated Injury of Human Pancreatic Acinar Cells and Acute Pancreatitis in 3 Mouse Models. Gastroenterology. 2015 Aug;149(2):481-92.e7.

[4]Ashmole I, et al. CRACM/Orai ion channel expression and function in human lung mast cells. J Allergy Clin Immunol. 2012 Jun;129(6):1628-35.e2

[5]Wen L, et al. Inhibitors of ORAI1 Prevent Cytosolic Calcium-Associated Injury of Human Pancreatic Acinar Cells and Acute Pancreatitis in 3 Mouse Models. Gastroenterology. 2015 Aug;149(2):481-92.e7

GSK-7975A 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.58mL

2.52mL

1.26mL

25.17mL

5.03mL

2.52mL

GSK-7975A 技术信息

CAS号1253186-56-9
分子式C18H12F5N3O2
分子量 397.299
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
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
动物实验配方

Tags: GSK-7975A | 1253186-56-9 | Calcium Channel | Ca2+ channels | Calcium Channel Inhibitor | Membrane Transporter/Ion Channel | Neuronal Signaling | Calcium Channel | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | GSK-7975A 纯度/质量文件 | GSK-7975A 生物活性 | GSK-7975A 参考文献 | GSK-7975A 实验方案 | GSK-7975A 技术信息

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