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TG100-115,677297-51-7

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  • ¥341 - 4180
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  • HY-10111
  • 2025年12月05日
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    • 详细信息
    • 文献和实验
    • 技术资料
    • 保存条件

      Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.

    • 库存

      货期:1-2天

    • 供应商

      MedChemExpress LLC

    • CAS号

      677297-51-7

    • 规格

      1 mg/5 mg/10 mg/25 mg/50 mg

    规格:1 mg产品价格:¥341.0
    规格:5 mg产品价格:¥848.0
    规格:10 mg产品价格:¥1246.0
    规格:25 mg产品价格:¥2620.0
    规格:50 mg产品价格:¥4180.0

    MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务。

    TG100-115

    CAS No. : 677297-51-7

    MCE 国际站:TG100-115

    产品活性:TG100-115 是一种选择性的 PI3Kγ/PI3Kδ 抑制剂,IC50 分别为 83 和 235 nM。

    研究领域:PI3K/Akt/mTOR

    作用靶点:PI3K

    In Vitro: TG100-115 inhibits PI3Kγ and PI3Kδ with IC50s of 83 and 235 nM, respectively, whereas both PI3Kα and PI3Kβ are relatively unaffected (IC50 values >1 μM). As a gauge of general specificity, TG100-115 is also assayed against a 133 protein kinase panel, none of which are inhibited at IC50 values <1 μM. TG100-115 potently inhibits edema and inflammation in response to multiple mediators known to participate in myocardial infarction, including vascular endothelial growth factor and platelet-activating factor; by contrast, endothelial cell mitogenesis, a repair process important to tissue survival after ischemic damage.

    In Vivo: 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.

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    图标文献和实验
    相关实验
    • 一种优化的PCR 方法——降落PCR 扩增目的基因

      / L ,MgCl2 115mmol/ L , dNTP012mmol/ L , Taq 018U ,第二轮: 取5 倍稀释的第一轮PCR 产物4μl 为模板, P7 、P8 各 0125μmol/ L ,MgCl2 115mmol/ L ,dNTP012mmol/ L ,Taq 018U 。分别在各灭菌PCR 管加入上述各反应成分,100 ℃煮沸5min ,立即冰浴5min , 加入 Taq DNA 聚合酶,混匀,离心,PCR 程序如下: 取10μl PCR 扩增产物,在2 %或3 %琼脂

    •  配对比较(t检验)时所需样本含量

      0.25         110         90       128 64     139 101 45 0.25 0.30       134 78       115 63     119 90 45   122 97 71 32 0.30 0.35     125 99 58     109 85 47   109 88 67 34   90 72 52 24 0.35 0.40   115 97 77 45   101 85 66 37 117 84 68 51 26 101 70 55

    •  PCR仪器的发展

      器 50×1.5ml or 50×1.5ml US $250. �plus US $ 15.-for Rack(x2) Techne PHC-1 PHC-2 Techne Ltd.(英) 变温铝块0~99℃三档 电热500W水冷100W 54×0.5ml 54×0.5ml 24×1.5ml £3383. � £3997. - BioOven BioThrm Corp(美) 变温气流 -150℃ 115V 11A 200’s

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