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Enalaprilat
Cat No.
CEI-0347
Description
Enalaprilat
CAS No.
84680-54-6
Molecular Weight
348.4
Purity
>99%
Storage
2 years at -20centigrade Powder
Targets
ACE
Molecular Formula
C18H24N2O5.2H2O
Solubility
DMSO 70 mg/mL, Water 5 mg/mL, Ethanol 1 mg/mL
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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