Sampatrilat

Modify Date: 2024-01-11 14:54:49

Sampatrilat Structure
Sampatrilat structure
Common Name Sampatrilat
CAS Number 129981-36-8 Molecular Weight 584.68200
Density 1.343g/cm3 Boiling Point N/A
Molecular Formula C26H40N4O9S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Sampatrilat


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].

 Names

Name (3R)-3-[[(2S)-6-amino-2-(methanesulfonamido)hexanoyl]amino]-4-[1-[[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]carbamoyl]cyclopentyl]butanoic acid
Synonym More Synonyms

 Sampatrilat Biological Activity

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[1][2].
Related Catalog
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 untreatedrats) 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]. Animal Model: Left coronary artery ligation (CAL) and sham-operated rats[2] Dosage: 30 mg/kg Administration: Oral adminstration Result: Prevented the increases in heart weight and cardiac collagen content of the rats with CAL.
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.

 Chemical & Physical Properties

Density 1.343g/cm3
Molecular Formula C26H40N4O9S
Molecular Weight 584.68200
Exact Mass 584.25200
PSA 240.58000
LogP 4.31350
Index of Refraction 1.584

 Safety Information

Hazard Codes Xi

 Synonyms

C26H40N4O9S
UK 81,252
sampatrilat
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