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  • ESI-09
    • ESI 09
    货号: abs817454
    CAS号: 263707-16-0
    分子式: C16H15ClN4O2
    分子量: 330.77
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs817454-5mg 1-2周 ¥741.00
    - +
    abs817454-10mg 1-2周 ¥1222.00
    - +
    abs817454-25mg 1-2周 ¥2078.00
    - +
    大包装询价
    产品描述
    描述

    ESI-09 is a specific exchange protein directly activated by cAMP (EPAC) inhibitor with IC50 of 3.2 μM and 1.4 μM for EPAC1 and EPAC2, respectively, >100-fold selectivity over PKA.

    纯度
    >98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    中文别名
    ESI 09
    外观
    faint yellow to dark orange powder
    可溶性/溶解性
    DMSO : 33.1 mg/mL (100 mM)

    Ethanol : 6.6 mg/mL (20 mM)
    生物活性
    靶点
    EPAC2 ,EPAC1
    In vitro(体外研究)
    ESI-09, a novel non-cyclic nucleotide EPAC antagonist, that is capable of specifically blocking intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic β cells. On the other hand, ESI-09 fails to suppress epidermal growth factor (EGF)-induced phosphorylation of Akt in AsPC1 cells. In pancreatic cancer cells, ESI-09 inhibits cells migration and invasion through decreasing 007-AM-induced cell adhesion dose-dependently. ESI-09 significantly reduces intracellular and total bacterial counts in human umbilical vein endothelial cells. ESI-09 effectively antagonizes Schwann cells (SC) differentiation induced by CPT-cAMP as well as the formation of myelin. In SC-neuron cultures, ESI-09 dramatically reduces the number of O1 positive and MBP positive SCs without compromising the health of the neurons or the SCs themselves.
    In vivo(体内研究)
    ESI-09 (10 mg/kg/d, i.p.), via pharmacological inhibition of EPAC1, protects WT C57BL/6 mice from fatal SFG rickettsiosis.
    参考文献
    参考文献
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