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Enalaprilat(hydrate)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Enalaprilat(hydrate)图片
CAS NO:84680-54-6
规格:98%
分子量:384.4
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Angiotensin-converting enzyme (ACE) converts angiotensin I to angiotensin II, a peptide hormone that impacts vascular smooth muscle tone and renal salt exchange, driving hypertension.
CAS:84680-54-6
分子式:C18H24N2O5.2H2O
分子量:384.4
纯度:98%
存储:Store at -20°C

Background:

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].


参考文献:
[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.