1253186-56-9
中文名称 | 1253186-56-9 |
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中文同义词 | 2,6-二氟-N-[1-[[4-羟基-2-(三氟甲基)苯基]甲基]-1H-吡唑-3-基]苯甲酰胺;化合物GSK-7975A;2,6-二氟-N-(1-(4-羟基-2-(三氟甲基)苄基)-1H-吡唑-3-基)苯甲酰胺 |
英文名称 | GSK-7975A |
英文同义词 | GSK-7975A;2,6-Difluoro-N-(1-{[4-hydroxy-2-(trifluoromethyl)phenyl]methyl} 1H-pyrazol-3-yl)benzamide;2,6-Difluoro-N-(1-(4-hydroxy-2-(trifluoromethyl)benzyl)-1H-pyrazol-3-yl)benzamide;Benzamide, 2,6-difluoro-N-[1-[[4-hydroxy-2-(trifluoromethyl)phenyl]methyl]-1H-pyrazol-3-yl]-;Ca channels,Calcium Channel,GSK 7975A,inhibit,Inhibitor,Ca2+ channels,GSK7975A,GSK-7975A |
CAS号 | 1253186-56-9 |
分子式 | C18H12F5N3O2 |
分子量 | 397.3 |
EINECS号 | |
相关类别 | |
Mol文件 | 1253186-56-9.mol |
结构式 |
1253186-56-9 性质
沸点 | 462.2±45.0 °C(Predicted) |
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密度 | 1.46±0.1 g/cm3(Predicted) |
储存条件 | 2-8°C |
溶解度 | DMSO:90.0(最大浓度 mg/mL);226.53(最大浓度 mM) |
酸度系数(pKa) | 8.82±0.20(Predicted) |
形态 | 固体 |
颜色 | 白色至米白色 |
GSK-7975A reduces FcεRI-dependent Ca 2+ influx and 3 μM GSK-7975A reduces the release of histamine, leukotriene C4, and cytokines (IL-5/-8/-13 and TNFα) by up to 50%. GSK-7975A inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety species. GSK-7975A completely inhibits calcium influx through CRAC channels. This leads to inhibition of the release of mast cell mediators and T-cell cytokines from multiple human and rat preparations. Mast cells from guinea-pig and mouse preparations are not inhibited by GSK-7975A; however cytokine release is fully blocked from T-cells in a mouse preparation. GSK-7975A inhibits toxin-induced activation of ORAI1 and/or activation of Ca 2+ currents after Ca 2+ release, in a concentration-dependent manner, in mouse and human pancreatic acinar cells (inhibition >90% of the levels observed in control cells). GSK-7975A also prevents activation of the necrotic cell death pathway in mouse and human pancreatic acinar cells.
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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-12507 | GSK-7975A | 1 mg | 400元 | |
2024/08/19 | HY-12507 | 1253186-56-9 GSK-7975A | 1253186-56-9 | 5mg | 850元 |