1253186-56-9
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- CAS号:
- 1253186-56-9
- 英文名:
- GSK-7975A
- 英文别名:
- GSK-7975A;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;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]-
- 中文名:
- 1253186-56-9
- 中文别名:
- 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;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
- CBNumber:
- CB73333733
- 分子式:
- C18H12F5N3O2
- 分子量:
- 397.3
- MOL File:
- 1253186-56-9.mol
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1253186-56-9化学性质
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沸点:
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462.2±45.0 °C(Predicted)
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密度:
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1.46±0.1 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMSO:90.0(Max Conc. mg/mL);226.53(Max Conc. mM)
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酸度系数(pKa):
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8.82±0.20(Predicted)
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形态:
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Solid
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颜色:
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White to off-white
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1253186-56-9性质、用途与生产工艺
GSK-7975A是高效有口服活性的 CRAC 通道抑制剂。
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.
1253186-56-9
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 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 |
1253186-56-9, 1253186-56-9 相关搜索:
- 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
- 化合物GSK-7975A
- 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
- 1253186-56-9
- Ca channels,Calcium Channel,GSK 7975A,inhibit,Inhibitor,Ca2+ channels,GSK7975A,GSK-7975A
- 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
- 2,6-Difluoro-N-(1-{[4-hydroxy-2-(trifluoromethyl)phenyl]methyl} 1H-pyrazol-3-yl)benzamide
- GSK-7975A