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• 产品描述： ESI-09 is a novel noncyclic nucleotide EPAC antagonist with IC50 values of 3.2 and 1.4 μM for EPAC1 and EPAC2, respectively.

• 靶点： IC50: 3.2 μM (EPAC1), 1.4 μM (EPAC2);cAMP; VirusProtease

• 体外研究：
  While cAMP competes with 8-NBD-cAMP binding with an IC50 of 39 µM, ESI-09 shows an increased potency with an apparent IC50 of 10 µM. ESI-09 inhibis cAMP-mediated EPAC2 and EPAC1 GEF activity with an IC50 of 1.4 and 3.2µM, respectively. ESI-09 could fit well into the functional cAMP-binding pocket of EPAC1, establishing favorable hydrophobic and hydrogen bonding interactions with the protein’s active-site residues. ESI-09 inhibits 007-AM-stimulated Akt phosphorylation at T308 and S473 in a dose-dependent manner. ESI-09 inhibits pancreatic cancer cells AsPC-1 and PANC-1 migration. ESI-09 inhibits EPAC1-mediated adhesion of PDA cells on collagen I. Exposure to ESI-09 significantly reduces intracellular and total bacterial counts in HUVECs at 30 min postinfection with 10 multiplicities of infection (MOI) of R. australis compared with similarly infected controls

• 体内研究：
  Treatment with ESI-09 dramatically protects WT mice against R. australis infection with much milder disease manifestations and significantly improves survival

• 参考文献：
  1. Almahariq M, et al. A novel EPAC-specific inhibitor suppresses pancreatic cancer cell migration and invasion. Mol Pharmacol. 2013 Jan;83(1):122-8. 2. Gong B, et al. Exchange protein directly activated by cAMP plays a critical role in bacterial invasion during fatal rickettsioses. Proc Natl Acad Sci U S A. 2013 Nov 26;110(48):19615-20.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.023 ml	15.116 ml	30.233 ml
  5 mM	0.605 ml	3.023 ml	6.047 ml
  10 mM	0.302 ml	1.512 ml	3.023 ml
  50 mM	0.06 ml	0.302 ml	0.605 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *