DX600 (trifluoroacetate salt)

DX600 is a potent and selective peptide inhibitor of angiotensin-converting enzyme 2 (ACE2; K_is = 2.8, 200, and 1,200 nM for recombinant, human, and murine ACE2, respectively).^1,2 ACE2 is an enzyme that is cardioprotective and renoprotective.³ Inhibition of ACE2 with DX600 reduces in vitro vascular repair by CD34⁺ stem/progenitor cells and exacerbates myocardial injury and dysfunction in vivo.^4,5

1.Huang, L., Sexton, D.J., Skogerson, K., et al.Novel peptide inhibitors of angiotensin-converting enzyme 2J. Biol. Chem.278(18)15532-15540(2003) 2.Joshi, S., Balasubramanian, N., Vasam, G., et al.Angiotensin converting enzyme versus angiotensin converting enzyme-2 selectivity of MLN-4760 and DX600 in human and murine bone marrow-derived cellsEur. J. Pharmacol.77425-33(2016) 3.Prada, J.A.H., Ferreira, A.J., Katovich, M.J., et al.Structure-based identification of small-molecule angiotensin-converting enzyme 2 activators as novel antihypertensive agentsHypertension511312-1317(2008) 4.Singh, N., Joshi, S., Guo, L., et al.ACE2/Ang-(1-7)/Mas axis stimulates vascular repair-relevant functions of CD34+ cellsAm. J. Physiol. Heart. Circ. Physiol.309H1697-H1707(2015) 5.Song, B., Zhang, Z.-Z., Zhong, J.-C., et al.Loss of angiotensin-converting enzyme 2 exacerbates myocardial injury via activation of the CTGF-fractalkine signaling pathwayCirc. J.77(12)2997-3006(2013)