1253186-56-9|2,6-Difluoro-N-(1-(4-hydroxy-2-(trifluoromethyl)benzyl)-1H-pyrazol-3-yl)benzamide|CsnPharm

CAS No.: 1253186-56-9

GSK-7975A Catalog No. CSN27221

Synonyms: GSK-7975

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

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400-920-2911

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生物活性

实验方案

技术信息

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].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5170 mL
- 12.5850 mL
- 25.1700 mL
- 5 mM
- 0.5034 mL
- 2.5170 mL
- 5.0340 mL
- 10 mM
- 0.2517 mL
- 1.2585 mL
- 2.5170 mL

技术信息

CAS号

1253186-56-9

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H12F5N3O2

运输

蓝冰

分子量

397.30

别名

GSK-7975

溶解度

DMSO	89.0 mg/mL (224.0 mM)

动物实验配方

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