Delapril HCl
产品说明书
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同义名 : | 盐酸地拉普利 ;Delapril Hydrochloride; Alindapril Hydrochloride; Delapril HCl, Delapril hydrochloride |
| CAS号 : | 83435-67-0 | |
| 货号 : | A189764 | |
| 分子式 : | C26H33ClN2O5 | |
| 纯度 : | 98% | |
| 分子量 : | 489.0 | |
| MDL号 : | MFCD00884619 | |
| 存储条件： |
Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 250 mg/mL(511.24 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 1.5 mg/mL(3.07 mM)，配合低频超声，并水浴加热至45℃助溶 |
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| 动物实验配方： |
| 生物活性 | |||
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| 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 (Cmax 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]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.04mL 0.41mL 0.20mL |
10.22mL 2.04mL 1.02mL |
20.45mL 4.09mL 2.04mL |
| 参考文献 |
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