Enalaprilat (hydrate) |
カタログ番号GC43601 |
アンジオテンシン変換酵素(ACE)は、血管平滑筋のトーンと腎臓の塩分交換に影響を与えるペプチドホルモンであるアンジオテンシンIIにアンジオテンシンIを変換し、高血圧を引き起こします。
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Cas No.: 84680-54-6
Sample solution is provided at 25 µL, 10mM.
Enalaprilat (dihydrate) (MK-422) is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 1.94 nM.
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].
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].
References:
[1]. Ceconi, C., et al., Angiotensin-converting enzyme (ACE) inhibitors have different selectivity for bradykinin binding sites of human somatic ACE. Eur J Pharmacol, 2007. 577(1-3): p. 1-6.
[2]. van Eickels, M., H. Vetter, and C. Grohe, Angiotensin-converting enzyme (ACE) inhibition attenuates insulin-like growth factor-I (IGF-I) induced cardiac fibroblast proliferation. Br J Pharmacol, 2000. 131(8): p. 1592-6.
[3]. Schumacher, J., et al., Effects of candesartan and enalaprilat on the organ-specific microvascular permeability during haemorrhagic shock in rats. Br J Anaesth, 2006. 96(4): p. 437-43.
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