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.
