GSK-7975A | Calcium Channel Inhibitor | AmBeed-信号通路专用抑制剂

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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 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]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JACS Au, 2024. Ambeed. [ A148168 ]; • JMC, 2024. Ambeed. [ A187643 ]; • JMC, 2024. Ambeed. [ A341145 , A633512 , A607865 , A167774 ]; • Biomacromolecules, 2024. Ambeed. [ A110759 ]; • Biomacromolecules, 2024. Ambeed. [ A203543 ]; 更多 >

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

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

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

摩尔计算器

计算溶液所需的质量，体积或浓度。 Ambeed 摩尔浓度计算器基于以下方程式：

浓度 (mol/L) × 体积 (L) × 分子量 (g/mol)=质量 (g)

浓度

体积

分子量

质量

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

GSK-7975A 纯度/质量文件产品仅供科研

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

GSK-7975A 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

GSK-7975A 质控信息

GSK-7975A 生物活性

GSK-7975A 参考文献

GSK-7975A 实验方案

GSK-7975A 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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GSK-7975A 纯度/质量文件产品仅供科研