In vitro
Enalaprilat has high affinity for human endothelial ACE with IC50 of 1.94 nM in vitro binding assay by displacing a saturating concentration of [125I]351A, a radiolabeled lisinopril analogue from ACE binding sites, and shows bradykiningiotensin I selectivity ratio of 1.00 calculated from double displacement experiments. Enalaprilat has the strong inhibitory effect on Abeta42-to-Abeta40-converting activity found in the N-domain of ACE, exhibiting a 10-fold lower IC50 (0.003~0.01 uM) than captopril (0.03~0.1 uM). Enalaprilat (100 nM) blocks protein kinase C epsilon by directly activating bradykinin B1 receptor at the canonical Zn2+ binding site, leading to prolonged nitric oxide (NO) production in cytokine-treated human lung microvascular endothelial cells.
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