89371-44-8
89371-44-8 结构式
基本信息
中文别名
咪达普利拉 英文别名
6366AIMIDAPRILAT
Imidaprilate
Imidapril Diacid
(4S)-3-[(2S)-N-[(1S)-1-Carboxy-3-phenylpropyl]alanyl]-1-methyl-2-oxo-4-imidazolidinecarboxylic acid
(4S)-3-{(2S)-2-[N-((1S)-1-Carboxy-3-phenylpropyl)amino]propionyl}-1-methyl-2-oxoimidazolidine-4-carboxylic Acid
物理化学性质
熔点180-1820C
比旋光度D19 -88.4° (c = 1 in 5% NaHCO3)
沸点592.1±60.0 °C(Predicted)
密度1.356±0.06 g/cm3(Predicted)
储存条件-20°C冷冻
溶解度可溶于酸性水溶液(轻微、加热、超声处理）、DMSO（轻微、加热）
酸度系数(pKa)2.17±0.10(Predicted)
形态固体
颜色白色至灰白色
常见问题列表
生物活性
Imidaprilate 是 TA-6366 的有效代谢物，为血管紧张素转化酶 (ACE) 抑制剂，可用于高血压的研究。靶点
IC50: 2.6 nM (ACE)
体外研究
Imidaprilate (6366A) is an active metabolite of 6366, acts as a potent angiotensin converting enzyme (ACE) inhibitor, with an IC 50 of 2.6 nM. Imidaprilate augments the bradykinin-induced contraction of guinea pig ileum, with AC 50 of 1.7 nM.
体内研究
Imidaprilate (≥0.2 mg/kg) inhibits angiotensin I (AT-I)-induced pressor response. TA-6366 lowers the blood pressure in two-kidney one-clip renal hypertensive rats at 0.5-2 mg/kg via oral administration, and in spontaneously hypertensive rats (SHRs) at 2 to 10 mg/kg.