Overview:

A potent, cell permeable Epac (exchange protein directly activated by cAMP) activator (1). Induces RAP1 activation and insulin secretion in pancreatic beta cell lines (2-5). Induces vascular relaxation in rate mesenteric artery (6). The acetoxymethyl ester confers increased cell-permeability and is cleaved by endogenous esterases to yield the active compound, 8-pCPT-2’-O-Me-cAMP. Addition to cell cultures should be done in serum-free media as esterases in the serum will cleave the acetoxymethyl ester and reduce cell permeability.

References:

1. MJ Vliem et al. Chembiochem. Sci.2008 9:2052.

2. OG Chepurny et al. J. Biol. Chem. 2009 284:10726.

3. GG Kelley et al. Islets 2009 1:260.

4. OG Chepurny et al. Am. J. Physiol. Edocrinol. Metab. 2010 298:E622.

5. I Dzhura et al Islets 2011 3:121.

6. OL Roberts et al. J. Physiol. 2013 591:5107.