Enalaprilat (dihydrate)

84680-54-6

C18H28N2O7

DMSO : >= 100 mg/mL (260.13 mM); H2O : 12.5 mg/mL (32.52 mM; Need ultrasonic)

Metabolic Enzyme/Protease; Autophagy

Enalaprilat (dihydrate) (MK-422) is an angiotensin-converting enzyme (ACE) inhibitor with IC₅₀ of 1.94 nM. IC50 & Target: ACE^[1]. 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 bradykinin/angiotensin I selectivity ratio of 1.00 calculated from double displacement experiments^[1]. Enalaprilat attenuates the IGF-I induced neonatal rat cardiac fibroblast growth (30% reduction) in a concentration-dependent fashion, with IC₅₀ of 90 mM^[2]. In Vivo: Administration of Enalaprilat induces a significant reduction of MAP at 70 minutes compared with the placebo group during haemorrhagic shock in rats, and results in a 50% reduction of CO, a general tendency of EB extravasation which is significant in the kidney and lungs, and a significant increase in ileal EB extravasation (53%)^[3].