生物活性 体外研究 体内研究 1253186-56-9 试剂级价格
ChemicalBook  CAS数据库列表  1253186-56-9

1253186-56-9

1253186-56-9,1253186-56-9,结构式
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
1253186-56-9化学性质
  • 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。
  • 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.

  • 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.

1253186-56-9上下游产品信息
上游原料
下游产品
1253186-56-9 试剂级价格
  • 更新日期:2024/08/19
  • 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:2024/08/19
  • 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
1253186-56-9生产厂家
  • 公司名称:TargetMol Chemicals Inc.
  • 联系电话:+1-781-999-5354 +1-00000000000
  • 电子邮件:marketing@targetmol.com
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