Description
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.
References
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 mouse 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
