1. Metabolic Enzyme/Protease
  2. Angiotensin-converting Enzyme (ACE)
    Neprilysin
  3. Sampatrilat

Sampatrilat (Synonyms: UK-81252)

Cat. No.: HY-123348
Handling Instructions

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.

For research use only. We do not sell to patients.

Sampatrilat Chemical Structure

Sampatrilat Chemical Structure

CAS No. : 129981-36-8

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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].

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].

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]
Dosage: 30 mg/kg
Administration: Oral adminstration
Result: Prevented the increases in heart weight and cardiac collagen content of the rats with CAL.
Molecular Weight

584.68

Formula

C₂₆H₄₀N₄O₉S

CAS No.

129981-36-8

SMILES

OC([[email protected]](CNC([[email protected]@H](NS(C)(=O)=O)CCCCN)=O)CC1(CCCC1)C(N[[email protected]](C(O)=O)CC2=CC=C(O)C=C2)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

SampatrilatUK-81252UK81252UK 81252Angiotensin-converting Enzyme (ACE)NeprilysinNeutral endopeptidaseNEPCluster of differentiation 10CD10BloodpressureregulationchronicheartfailureCHFnACEcACEvasopeptidasecardiaccollagenCALInhibitorinhibitorinhibit

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Sampatrilat
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