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| | 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 | | EINECS: | | | Product Categories: | | | 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 | | InChI | 1S/C18H12F5N3O2/c19-13-2-1-3-14(20)16(13)17(28)24-15-6-7-26(25-15)9-10-4-5-11(27)8-12(10)18(21,22)23/h1-8,27H,9H2,(H,24,25,28) | | InChIKey | CPYTVBALBFSXSH-UHFFFAOYSA-N | | SMILES | FC(F)(F)c1c(ccc(c1)O)C[n]2nc(cc2)NC(=O)c3c(cccc3F)F |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | 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 |
| | GSK-7975A Preparation Products And Raw materials |
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