| Description | Sampatrilat is an effecive and orally active vasopeptidase inhibitor of ACE and neutral endopeptidase. Sampatrilat inhibits C-domain ACE (Ki=13.8 nM) 12.4-fold more potent than that for the N-domain (Ki=171.9 nM). |
| In vivo | Sampatrilat (p.o.; 30 mg/kg; once a day; 5 weeks) decreases the mortality of the rats with CAL (20% versus 57% for untreated rats) and increase in the survival rate and improvement of the hemodynamic function of the rats with CAL [2]. |
| Target activity | nACE:171.9 nM(ki), CACE:(ki)13.8 nM |
| Synonyms | UK-81252 |
| molecular weight | 584.68 |
| Molecular formula | C26H40N4O9S |
| CAS | 129981-36-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Sharma RK, et al. The Dynamic Nonprime Binding of Sampatrilat to the C-Domain of Angiotensin-Converting Enzyme. J Chem Inf Model. 2016 Dec 27;56(12):2486-2494. 2. Maki T, et al. Beneficial effects of sampatrilat, a novel vasopeptidase inhibitor, on cardiac remodeling and function of rats with chronic heart failure following left coronary artery ligation.J Pharmacol Exp Ther. 2003 Apr;305(1):97-105. |