| Identification | Back Directory | [Name]
GSK-7975A | [CAS]
1253186-56-9 | [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]- | [Molecular Formula]
C18H12F5N3O2 | [MDL Number]
MFCD28411366 | [MOL File]
1253186-56-9.mol | [Molecular Weight]
397.3 |
| Chemical Properties | Back Directory | [Boiling point ]
462.2±45.0 °C(Predicted) | [density ]
1.46±0.1 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMSO:90.0(Max Conc. mg/mL);226.53(Max Conc. mM) | [form ]
Solid | [pka]
8.82±0.20(Predicted) | [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 |
| Hazard Information | Back Directory | [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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| Company Name: |
cjbscvictory
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| Tel: |
13348960310 13348960310; |
| Website: |
https://www.weikeqi-biotech.com/ |
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