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ESI 09 is a ePAC inhibitor with IC50 values of 3.2 and 1.4 μM for EPAC1 and EPAC2, respectively. ESI-09 inhibits EPAC-mediated insulin releases from pancreatic β cells. Selective for EPAC over PKA. ESI-09 decreases migration and invasion of AsPc-1 and PANC-1 pancreatic cancer cells in vitro.
| Cell Experiment | |
|---|---|
| Cell lines | Porcine coronary artery SMCs |
| Preparation method | Porcine coronary artery SMCs were serum deprived for 24 hours and then treated with: 0.01% DMSO as solvent control; 007 (50 μM); G-1 (1 μM); G-1(1 μM) + ESI-09 (10 μM) and PKI (5 μM). |
| Concentrations | 10 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Male and female C57BL/6J mice |
| Formulation | Corn oil |
| Dosages | 20 mg/kg |
| Administration | Oral gavage |
| Molecular Weight | 330.77 |
| Formula | C16H15ClN4O2 |
| CAS Number | 263707-16-0 |
| Form | Solid |
| Solubility (25°C) | DMSO 35 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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