8-pCPT-2-O-Me-cAMP-AM (1152197-23-3) is 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 rat 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 serum will cleave the acetoxymethyl ester and reduce cell permeability.
1) Vliem et al. (2008), 8-pCPT-2'-O-Me-cAMP-AM: an improved Epac-selective cAMP analogue; Chem. Biochem., 9 2052
2) Chepurny et al. (2009), Enhanced Rap1 activation and insulin secretagogue properties of an acetoxymethyl ester of an Epac-selective cyclic AMP analog in rat INS-1 cells: studies with 8-pCPT-2'-O-Me-cAMP-AM; J. Biol. Chem., 284 10728
3) Kelley et al. (2009), Glucose-dependent potentiation of mouse islet insulin secretion by Epac activator 8-pCPT-2'-O-Me-cAMP-AM; Islets, 1 260
4) Chepurny et al. (2010), PKA-dependent potentiation of glucose-stimulated insulin secretion by Epac activator 8-pCPT-2'-O-Me-cAMP-AM in human islets of Langerhans; Am. J. Physiol. Endocrinol. Metab., 298 E622
5) Dzhura et al. (2011), Phospholipase C-ε links EPAC2 activation to the potentiation of glucose stimulated insulin secretion from moused islets of Langerhans; Islets, 3 121
6) Roberts et al. (2013), Exchange protein activated by cAMP (Epac) induces vascular relaxation by activating Ca2+-sensitive K+ channels in rat mesenteric artery; J. Physiol., 591 5107