1253186-56-9
- CAS号:1253186-56-9
- 英文名:GSK-7975A
- 中文名:1253186-56-9
- CBNumber:CB73333733
- 分子式:C18H12F5N3O2
- 分子量:397.3
- MOL File:1253186-56-9.mol
- 沸点 :462.2±45.0 °C(Predicted)
- 密度 :1.46±0.1 g/cm3(Predicted)
- 储存条件 :2-8°C
- 溶解度 :DMSO:90.0(Max Conc. mg/mL);226.53(Max Conc. mM)
- 酸度系数(pKa) :8.82±0.20(Predicted)
- 形态 :Solid
- 颜色 :White to off-white
1253186-56-9性质、用途与生产工艺
- 生物活性 GSK-7975A是高效有口服活性的 CRAC 通道抑制剂。
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体外研究
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.
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体内研究
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.
- 更新日期:2024/11/08
- 产品编号:HY-12507
- 产品名称:GSK-7975A
- CAS编号:
- 包装:1 mg
- 价格:400元
- 更新日期:2024/11/08
- 产品编号:HY-12507
- 产品名称:1253186-56-9 GSK-7975A
- CAS编号:1253186-56-9
- 包装:5mg
- 价格:850元
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