Enalaprilat-dihydrate-MK-422-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEnalaprilat dihydrateCat. No.: HY-B0231CAS No.: 84680-54-6Synonyms: MK-422分式: CHNO分量: 384.42作靶点: Angiotensin-converting Enzyme (ACE); Autophagy作通路: Metabolic Enzyme/Protease; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent

2、 -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (260.13 mM)H2O : 12.5 mg/mL (32.52 mM; Need ultrasonic)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.6013 mL 13.0066 mL 26.0132 mL5 mM 0.5203 mL 2.6013 mL 5.2026 mL10 mM 0.2601 mL 1.3007 mL 2.6013 mL请

3、根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.50 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90%

4、corn oil1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (6.50 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Enalaprilat (dihydrate) (MK-422)管紧张素转化酶 (ACE) 抑制剂，IC50 为 1.94 nM。IC50 & Target ACE 1.体外研究 Enalaprilat has high affinity for human endothelial ACE with IC50 of 1.94 nM in vit

5、ro binding assay bydisplacing a saturating concentration of 125I351A, a radiolabeled lisinopril analogue from ACE binding sites,and shows bradykinin/angiotensin I selectivity ratio of 1.00 calculated from double displacement experiments1. Enalaprilat attenuates the IGF-I induced neonatal rat cardiac

6、 fibroblast growth (30% reduction) in aconcentration-dependent fashion, with IC50 of 90 mM 2.体内研究 Administration of Enalaprilat induces a significant reduction of MAP at 70 minutes compared with the placebogroup during haemorrhagic shock in rats, and results in a 50% reduction of CO, a general tende

7、ncy of EBextravasation which is significant in the kidney and lungs, and a significant increase in ileal EB extravasation(53%) 3.REFERENCES1. Ceconi, C., et al., Angiotensin-converting enzyme (ACE) inhibitors have different selectivity for bradykinin binding sites of humansomatic ACE. Eur J Pharmaco

8、l, 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 haemorrhagicshock in rats. Br J Anaesth, 2006. 96(4): p. 437-43.McePdfHeightCaution: Product has not been fully validated for medical appli