1、Product Data SheetEnalaprilat dihydrateCat. No.: HY-B0231CAS No.: 84680-54-6分式: CHNO分量: 384.42作靶點: Angiotensin-converting Enzyme (ACE); Autophagy作通路: Metabolic Enzyme/Protease; Autophagy儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 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制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6

3、months; -20C, 1 month。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility

4、: 2.5 mg/mL (6.50 mM); Clear solution此案可獲得 2.5 mg/mL (6.50 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.50 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得

5、2.5 mg/mL (6.50 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Enalaprilat dihydrate (MK-422)管緊張素轉(zhuǎn)化酶 (ACE) 抑制劑，IC50 為 1.94 nM。IC & Target ACE1.體外研究 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.體內(nèi)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