ESI-05 (Synonyms: NSC 116966)
目录号: PL11766 纯度: ≥99%
CAS No. :5184-64-5
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中文名称
ESI-05
英文名称
ESI-05
英文别名
Benzene,1,3,5-trimethyl-2-[(4-methylphenyl)sulfonyl]-;1,3,5-trimethyl-2-(4-methylphenyl)sulfonylbenzene;AC1L6RWH;AC1Q6TOK;CHEMBL2313653;CTK4J4972;mesityl(4-methylphenyl) sulfone;MolPort-002-893-280;NSC116966;SureCN9001218;1,3,5-Trimethyl-2-[(4-methylphenyl)sulfonyl]-benzene;Mesityl (4-methylphenyl) sulfone;ESI-05
Cas No.
5184-64-5
分子式
C16H18O2S
分子量
274.38
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
ESI-05 是一种特异性 EPAC2 抑制剂。ESI-05 抑制 cAMP 介导的 EPAC2 GEF 活性,IC50 值为 0.43 μM。ESI-05 可用于糖尿病、胰岛素分泌和神经系统疾病的研究。
生物活性
ESI-05 is a specific exchange proteins directly activated by cAMP 2 (EPAC2) inhibitor. ESI-05 inhibits cAMP-mediated EPAC2 GEF activity with an IC 50 of 0.43 μM. ESI-05 can be used for the research of diabetes, insulin secretion and neurological disorders.
性状
Solid
IC50 & Target[1][2]
IC50: 0.43 μM (EPAC2)
体外研究(In Vitro)
ESI-05 (0.01 μM -1 nM) inhibits cAMP-mediated EPAC2 GEF activity with IC50 of 0.43 μM, but completely ineffective in suppressing EPAC1 GEF activity.
ESI-05 (1, 5, 10, and 25 μM; 5 min) selectively modulates EPAC2 activation in living cells. has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis
体内研究(In Vivo)
ESI-05 (2, 4, and 8 mg/kg) decreases neuronal apoptosis by inhibiting the p38/BIM pathway in vivo. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Intracranial hemorrhage (ICH) model
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Tsalkova T, et al. Isoform-specific antagonists of exchange proteins directly activated by cAMP. Proc Natl Acad Sci U S A. 2012 Nov 6;109(45):18613-8.
[2]. Yan Zhuang, et al. Inhibition of EPAC2 Attenuates Intracerebral Hemorrhage-Induced Secondary Brain Injury via the p38/BIM/Caspase-3 Pathway. J Mol Neurosci. 2019 Mar;67(3):353-363.
溶解度数据
In Vitro: DMSO : 50 mg/mL (182.23 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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