ESI-09 is a novel noncyclic nucleotideEPACantagonist withIC₅₀values of 3.2 and 1.4 μM for EPAC1 and EPAC2, respectively.

IC50: 3.2 μM (EPAC1), 1.4 μM (EPAC2)^[1]

While cAMP competes with 8-NBD-cAMP binding with an IC₅₀of 39 μM, ESI-09 shows an increased potency with an apparent IC₅₀of 10 μM. ESI-09 inhibis cAMP-mediated EPAC2 and EPAC1 GEF activity with an IC₅₀of 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^[1]. Exposure to ESI-09 significantly reduces intracellular and total bacterial counts in HUVECs at 30 min postinfection with 10 multiplicities of infection (MOI) ofR. australiscompared with similarly infected controls^[2].

Treatment with ESI-09 dramatically protects WT mice againstR. australisinfection with much milder disease manifestations and significantly improves survival^[2].

330.77

Solid

C₁₆H₁₅ClN₄O₂

263707-16-0

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 47 mg/mL(142.09 mM)

*"≥" means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.5 mg/mL (7.56 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.56 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (7.56 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.56 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。