|2-((S)-N-(2,3-二氢-1H-茚-2-基)-2-(((S)-1-乙氧基-1-氧代-4-苯基丁烷-2-基)氨基)丙酰胺)乙酸盐酸盐|CsnPharm

CAS No.: 83435-67-0

Delapril HCl/地拉普利盐酸盐 Catalog No. CSN23248

Synonyms: Delapril HCl;地拉普利盐酸盐

Delapril HCl is an ester prodrug which can inhibit the activity of angiotensin I converting enzyme in the blood. It is an antihypertensive effect.

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技术信息

生物活性

描述The results of worldwide clinical studies indicate that angiotensin converting enzyme (ACE) inhibitors, exemplified by Captopril and enalapril, are very useful for treatment of hypertension. Delapril HCl, the hydrochloride salt form of delapril, is a lipophilic, non-sulfhydryl ACE inhibitor with antihypertensive activity^[1]. In dogs given 10 mg/kg of [¹⁴C]delapril, 72% of the dose was absorbed. Plasma levels of M-I (an active metabolite of delapril) peaked within 0.4 hour of administration (C_max 0.9 μg/mL), then declined biphasically with half-lives of 0.3 and 2.8 hours. When delapril (3 mg/kg) is administered orally to spontaneously hypertensive rats (SHR) for 2 weeks, the tissue ACE inhibitory activity, especially on aortic wall vascular ACE, was more marked than captopril (30 mg/kg) and enalapril (3 mg/kg), whereas all inhibitors were about equally effective on plasma ACE. Moreover, the effect of delapril on tissue ACE lasted longer than on the circulatory system. At oral doses of 1-10 mg/kg, delapril exerted marked and long-lasting antihypertensive action in RAS-dependent models of hypertension, such as 2-kidney, l-clip hypertensive rats and dogs. In stroke-prone SHR and in SHR with chronic renal failure, delapril (10 and 30 mg/kg/day orally for 32 and 28 days, respectively) was also able to improve survival rate significantly and prevented the development of symptoms of cardiac and renal injury, such as stroke, cardiac hypertrophy, and renal sclerosis^[2].
参考文献

[1] Saruta T, Nishikawa K. Characteristics of a new angiotensin converting enzyme inhibitor: delapril. Am J Hypertens. 1991;4(1 Pt 2):23S‐28S
[2] Razzetti R, Acerbi D. Pharmacokinetic and pharmacologic properties of delapril, a lipophilic nonsulfhydryl angiotensin-converting enzyme inhibitor. Am J Cardiol. 1995;75(18):7F-12F

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0450 mL
- 10.2249 mL
- 20.4497 mL
- 5 mM
- 0.4090 mL
- 2.0450 mL
- 4.0899 mL
- 10 mM
- 0.2045 mL
- 1.0225 mL
- 2.0450 mL

技术信息

CAS号

83435-67-0

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H33ClN2O5

运输

蓝冰

分子量

489.00

别名

Delapril HCl;地拉普利盐酸盐

溶解度

DMSO	190.0 mg/mL (388.5 mM)
Water	insoluble

动物实验配方

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