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S80889

TG100-115

源叶(MedMol) 98%
  • 英文名:
  • TG100-115
  • 别名:
  • 6,7-Bis(3-hydroxyphenyl)pteridine-2,4-diamine
  • CAS号:
  • 677297-51-7
  • 分子式:
  • C18H14N6O2
  • 分子量:
  • 346.35
  • 核磁/质谱:
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S80889-1mg 98% ¥170.00元 10 - - - EA 加入购物车
源叶(MedMol) S80889-5mg 98% ¥595.00元 6 - - - EA 加入购物车
源叶(MedMol) S80889-10mg 98% ¥990.00元 8 - - - EA 加入购物车
源叶(MedMol) S80889-25mg 98% ¥1980.00元 6 - - - EA 加入购物车
源叶(MedMol) S80889-50mg 98% ¥3400.00元 预计交期:2-3天 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: TG100-115 is a selective PI3Kγ/PI3Kδ inhibitor with IC50s of 83 and 235 nM, respectively.
  • 靶点: PI3Kδ:235 nM (IC50);PI3Kγ:83 nM (IC50);PI3K
  • 体内研究:
    To correlate these in vivo responses with the molecular target of interest, PI3K pathway signaling is monitored through western blot analyses of Akt phosphorylation (a PI3K-mediated event). VEGF injection i.v. in mice induces a rapid Akt phosphorylation readily detectable in lung lysates, pretreatment with TG100-115 blocks this response. Blockade is seen with TG100-115 doses as low as 0.5 mg/kg and persists over a period of several hours. In initial dose-ranging studies, generally equivalent responses are observed using TG100-115 doses of 0.5-10 mg/kg, and we therefore elected to conduct a statistically powered test at the lowest dose. Animals dosed with TG100-115 as a single 0.5 mg/kg i.v. bolus 30 min after reperfusion developed smaller infarcts vs. vehicle-treated controls. Measuring infarct area as percent of total LV ischemic area, infarct size is reduced by 35% (P=0.04). Viable tissue within the ischemic zone is increased by 37% (P=0.04), directly demonstrating the cardioprotective effect of PI3Kγ/δ inhibition
  • 参考文献:
    1. Doukas J, et al. Phosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury. Proc Natl Acad Sci U S A. 2006 Dec 26;103(52):19866-71.
  • 溶解性: DMSO  :  33.33  mg/mL  (96.23  mM;  ultrasonic  and  warming  and  adjust  pH  to  2  with  HCl  and  heat  to  60°C)
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.887 ml 14.436 ml 28.873 ml
    5 mM 0.577 ml 2.887 ml 5.775 ml
    10 mM 0.289 ml 1.444 ml 2.887 ml
    50 mM 0.058 ml 0.289 ml 0.577 ml
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