GSK-7975A
GSK-7975A Basic information
- Product Name:
- GSK-7975A
- Synonyms:
-
- GSK-7975A
- 2,6-Difluoro-N-(1-{[4-hydroxy-2-(trifluoromethyl)phenyl]methyl} 1H-pyrazol-3-yl)benzamide
- Benzamide, 2,6-difluoro-N-[1-[[4-hydroxy-2-(trifluoromethyl)phenyl]methyl]-1H-pyrazol-3-yl]-
- 2,6-Difluoro-N-(1-(4-hydroxy-2-(trifluoromethyl)benzyl)-1H-pyrazol-3-yl)benzamide
- Ca channels,Calcium Channel,GSK 7975A,inhibit,Inhibitor,Ca2+ channels,GSK7975A,GSK-7975A
- GSK-7975A, 10 mM in DMSO
- CRAC Channel Inhibitor IV, GSK-7975A
- CAS:1253186-56-9
- CAS:
- 1253186-56-9
- MF:
- C18H12F5N3O2
- MW:
- 397.3
- Mol File:
- 1253186-56-9.mol
GSK-7975A Chemical Properties
- Boiling point:
- 462.2±45.0 °C(Predicted)
- Density
- 1.46±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMSO:90.0(Max Conc. mg/mL);226.53(Max Conc. mM)
- pka
- 8.82±0.20(Predicted)
- form
- Solid
- color
- White to off-white
GSK-7975A Usage And Synthesis
Uses
GSK-7975A is a potent and orally available CRAC channel inhibitor.
Biological Activity
Cell permeable: yes', 'Primary Target
CRAC', 'Reversible: yes
in vivo
GSK-7975A inhibits local and systemic features of acute pancreatitis in TLCS-AP, CER-AP, FAEE-AP, in dose- and time-dependent manners.? GSK-7975A significantly reduces increases in serum amylase, IL6, and pancreatic MPO levels; lung MPO is reduced significantly by low dose only. GSK-7975A markedly reduces pancreatic histopathology in TLCS-AP, CER-AP, and FAEE-AP[3].
References
[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. DOI:10.1016/j.jaci.2012.01.070
[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. DOI:10.1016/j.ejphar.2013.02.022
[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. DOI:10.1053/j.gastro.2015.04.015
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