129981-36-8
129981-36-8 structure
- Name: Sampatrilat
- Chemical Name: (3R)-3-[[(2S)-6-amino-2-(methanesulfonamido)hexanoyl]amino]-4-[1-[[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]carbamoyl]cyclopentyl]butanoic acid
- CAS Number: 129981-36-8
- Molecular Formula: C26H40N4O9S
- Molecular Weight: 584.68200
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Angiotensin-converting Enzyme (ACE)
- Create Date: 2018-04-30 08:00:00
- Modify Date: 2024-01-11 14:54:49
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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].
| Name | (3R)-3-[[(2S)-6-amino-2-(methanesulfonamido)hexanoyl]amino]-4-[1-[[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]carbamoyl]cyclopentyl]butanoic acid |
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| Synonyms |
C26H40N4O9S
UK 81,252 sampatrilat |
| 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]. |
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| 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 |
| 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 |
| Hazard Codes | Xi |
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