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Sampatrilat
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Sampatrilat图片
CAS NO:129981-36-8
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
UK-81252
产品介绍
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。
生物活性

Sampatrilat (UK-81252) is a potent and orally activevasopeptidaseinhibitor ofACEand 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]

体内研究
(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].

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.
分子量

584.68

Formula

C26H40N4O9S

CAS 号

129981-36-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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