MedChemExpress -Model Sampatrilat -129981-36-8

FromMedChemExpress LLC (MCE)

Sampatrilat (UK-81252) is a potent and orally active vasopeptidase inhibitor of ACE and neutral endopeptidase (NEP). Sampatrilat inhibits C-domain ACE (Ki=13.8 nM) 12.4-fold more potent than that for the N-domain (Ki=171.9 nM). Sampatrilat (UK-81252) can be used for the study of chronic heart failure and blood pressure regulation[1][2].

Sampatrilat

MCE China：Sampatrilat

Brand：MedChemExpress (MCE)

Cat. No.HY-123348

CAS：129981-36-8

Synonyms：UK-81252

Purity：99.22%

Storage：-20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Sampatrilat (UK-81252) is a potent and orally active vasopeptidase inhibitor of ACE and neutral endopeptidase (NEP). Sampatrilat inhibits C-domain ACE (Ki=13.8 nM) 12.4-fold more potent than that for the N-domain (Ki=171.9 nM). Sampatrilat (UK-81252) can be used for the study of chronic heart failure and blood pressure regulation.

In Vivo：Sampatrilat (oral adminstration; 30 mg/kg; once a day; 5 weeks) reduces the mortality of the rats with CAL (20% versus 57% for untreated rats) and increase in the survival rate and improvement of hemodynamic function of the rats with CAL. This compound suppresses tissue ACE and neutral endopeptidase (NEP) activities, but it does not affect the arterial blood pressure, whereas it attenuates the CAL-induced increases in the left ventricular end-diastolic pressure, heart weight, and collagen content of the viable left Ventricle[2].

IC50 & Target：Ki: 13.8 nM (cACE); 171.9 nM (nACE)[1] In Vivo Sampatrilat (oral adminstration; 30 mg/kg; once a day; 5 weeks) reduces the mortality of the rats with CAL (20% versus 57% for untreated rats) and increase in the survival rate and improvement of hemodynamic function of the rats with CAL. This compound suppresses tissue ACE and neutral endopeptidase (NEP) activities, but it does not affect the arterial blood pressure, whereas it attenuates the CAL-induced increases in the left ventricular end-diastolic pressure, heart weight, and collagen content of the viable left Ventricle[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Left coronary artery ligation (CAL) and sham-operated rats[2]

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. [Content Brief]

[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. [Content Brief]

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