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Enalaprilat Dihydrate

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Chemical Structure| 84680-54-6 同义名 : 依那普利拉二水合物 ;MK-422;Enalaprilat (hydrate);MK-422 Dihydrate
CAS号 : 84680-54-6
货号 : A502548
分子式 : C18H28N2O7
纯度 : 97%
分子量 : 384.424
MDL号 : MFCD00941393
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(273.14 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 12 mg/mL(31.22 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • ACE

    ACE, IC50:1.94 nM
描述 Enalaprilat dihydrate (MK-422) is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 1.94 nM. The ACE inhibitors generally had higher affinity for the bradykinin than the angiotensin I binding sites. Perindoprilat had the highest selectivity for bradykinin versus angiotensin I binding sites, and enalaprilat has the lowest[3]. Enalaprilat attenuates the IGF-I induced neonatal rat cardiac fibroblast growth (30% reduction) in a concentration-dependent fashion, with IC50 of 90 mM[4]. The combination with candesartan in nephrotic rats significantly changed the pharmacokinetics of enalaprilat, showing increased accumulation and decreased elimination[5]. Intracoronary enalaprilat improves coronary microvascular function and protects myocardium from procedure-related injury in patients with coronary artery disease undergoing PCI (percutaneous coronary intervention) [6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.60mL

0.52mL

0.26mL

13.01mL

2.60mL

1.30mL

26.01mL

5.20mL

2.60mL
参考文献

[1]Zou K, Maeda T, et al. Abeta42-to-Abeta40- and angiotensin-converting activities in different domains of angiotensin-converting enzyme. J Biol Chem. 2009 Nov 13;284(46):31914-20.

[2]Ceconi C, Francolini G, et al. Angiotensin-converting enzyme (ACE) inhibitors have different selectivity for bradykinin binding sites of human somatic ACE. Eur J Pharmacol. 2007 Dec 22;577(1-3):1-6. Epub 2007 Aug 3.

[3]Ceconi C, Francolini G, Olivares A, Comini L, Bachetti T, Ferrari R. Angiotensin-converting enzyme (ACE) inhibitors have different selectivity for bradykinin binding sites of human somatic ACE. Eur J Pharmacol. 2007 Dec 22;577(1-3):1-6

[4]van Eickels M, Vetter H, Grohé C. Angiotensin-converting enzyme (ACE) inhibition attenuates insulin-like growth factor-I (IGF-I) induced cardiac fibroblast proliferation. Br J Pharmacol. 2000 Dec;131(8):1592-6

[5]Schumacher J, Puchakayala MR, Binkowski K, Eichler W, Dendorfer A, Klotz KF. Effects of candesartan and enalaprilat on the organ-specific microvascular permeability during haemorrhagic shock in rats. Br J Anaesth. 2006 Apr;96(4):437-43

[6]Mangiacapra F, Peace AJ, Di Serafino L, Pyxaras SA, Bartunek J, Wyffels E, Heyndrickx GR, Wijns W, De Bruyne B, Barbato E. Intracoronary EnalaPrilat to Reduce MICROvascular Damage During Percutaneous Coronary Intervention (ProMicro) study. J Am Coll Cardiol. 2013 Feb 12;61(6):615-21