山帕曲拉
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- CAS号:
- 129981-36-8
- 英文名:
- sampatrilat
- 英文别名:
- UK-81252;sampatrilat;L-Tyrosine, N2-(methylsulfonyl)-L-lysyl-1-[(2S)-3-amino-2-carboxypropyl]cyclopentanecarbonyl-
- 中文名:
- 山帕曲拉
- 中文别名:
- 山帕曲拉;化合物 T16840
- CBNumber:
- CB61374083
- 分子式:
- C26H40N4O9S
- 分子量:
- 584.687
- MOL File:
- 129981-36-8.mol
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山帕曲拉化学性质
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形态:
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Solid
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颜色:
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White to off-white
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山帕曲拉性质、用途与生产工艺
Sampatrilat (UK-81252) 是一种强效具有口服活性的血管肽酶抑制剂，可抑制血管紧张素转换酶 (ACE) 和中性血管内肽酶 (NEP)。Sampatrilat 对 C-domain ACE (Ki=13.8 nM) 的抑制作用是 N-domain 的 12.4 倍 (Ki=171.9 nM)。Sampatrilat (UK-81252) 可用于慢性心力衰竭和血压调节的相关研究。
Ki: 13.8 nM (cACE); 171.9 nM (nACE)
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.
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Animal Model:
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Left coronary artery ligation (CAL) and sham-operated rats
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Dosage:
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30 mg/kg
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Administration:
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Oral adminstration
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Result:
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Prevented the increases in heart weight and cardiac collagen content of the rats with CAL.
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山帕曲拉
上下游产品信息
上游原料
下游产品
129981-36-8, 山帕曲拉 相关搜索:
- C26H40N4O9S
- 化合物 T16840
- 山帕曲拉
- 129981-36-8
- L-Tyrosine, N2-(methylsulfonyl)-L-lysyl-1-[(2S)-3-amino-2-carboxypropyl]cyclopentanecarbonyl-
- UK-81252
- sampatrilat