依那普利拉二水合物作用机制 - Medchemexpress - MCE中国

1、Product Data SheetEnalaprilat dihydrateCat. No.: HY-B0231CAS No.: 84680-54-6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 -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (260.13 mM)H2O :

2、12.5 mg/mL (32.52 mM; Need ultrasonic)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6

3、months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。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。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility

4、: 2.5 mg/mL (6.50 mM); Clear solution此案可获得 2.5 mg/mL (6.50 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.50 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得

5、2.5 mg/mL (6.50 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Enalaprilat dihydrate (MK-422)管紧张素转化酶 (ACE) 抑制剂，IC50 为 1.94 nM。IC & Target ACE1.体外研究 Enalaprilat has high affinity for human endothelial ACE with IC50 of 1.94 nM in vi

6、tro binding assay by displacing asaturating concentration of 125I351A, a radiolabeled lisinopril analogue from ACE binding sites, and showsbradykinin/angiotensin I selectivity ratio of 1.00 calculated from double displacement experiments1. Enalaprilatattenuates the IGF-I induced neonatal rat cardiac

7、 fibroblast growth (30% reduction) in a concentration-dependentfashion, with IC50 of 90 mM2.体内研究 Administration of Enalaprilat induces a significant reduction of MAP at 70 minutes compared with the placebo groupduring haemorrhagic shock in rats, and results in a 50% reduction of CO, a general tenden

8、cy of EB extravasation 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 human somatic ACE. Eur JPharmaco

9、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 cardiacfibroblast 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 JAnaesth, 2006. 96(4): p. 437-43.McePdfHeightCaution: Product has not been fully validated for medical applicatio