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- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
- 英文名:
Perindopril tert-butylamine salt;S-9490 erbumine
- 库存:
99
- 供应商:
爱必信(上海)生物科技有限公司
- CAS号:
107133-36-8
- 规格:
500mg/100mg
| 规格: | 500mg | 产品价格: | ¥1650.0 |
|---|---|---|---|
| 规格: | 100mg | 产品价格: | ¥550.0 |
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抑制剂描述: 产品名称:Perindopril Erbumine 产品别名:见爱必信官网 英文别名:Perindopril Erbumine 靶点:ACE CAS:107133-36-8 纯度:99% 外观:见爱必信官网 保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. 描述: Perindopril erbumine 是长效血管紧张素转换酶(ACE)抑制剂。 溶解性:Ethanol : 22.1 mg/mL (50 mM) 体外研究: Perindopril Erbumine displays a higher binding affinity for the bradykinin binding sites than the angiotensin I binding sites of the angiotensin-converting enzyme (ACE) with bradykinin/angiotensin I selectivity ratio of 1.44. Perindopril Erbumine inhibits the angiotensin- and Aβ42-to-Aβ40-converting activity of mutated ACE containing two active domains (F-ACE) with IC50 of 0.03-0.1 μM, and 0.01-0.03 μM, respectively. Perindopril Erbumine (~2 μM) displays no significant cytotoxicity towards SCC-VII and KB cells, but can significantly reduce the production of angiotensin II and the transcription of VEGF in KB cells in a concentration-dependent manner. 体内研究:Oral administration of Perindopril Erbumine at 2 mg/kg/day has a significant inhibitory effect on SCC-VII tumor growth, and reduces blood vessel formation surrounding the tumors in vivo due to the suppression of VEGF-induced angiogenesis. Administration of Perindopril Erbumine at 2 mg/kg/day displays a strong inhibitory effect of the BNL-HCC tumor growth in rats similar to that of 20 mg/kg/day and in contrast to the AT1-R antagonist candesartan or losartan which at the dose of 20 mg/kg/day has no inhibitory effect. Administration of Perindopril Erbumine at 3 mg/kg/day significantly inhibits LPS-induced apoptosis by 6.4% in RAECs in vivo than that of ramipril by 3.2%. Administration of Perindopril Erbumine (1 mg/kg/day) significantly suppresses the hippocampal ACE activity, and prevents cognitive impairment and brain injury in rats with Alzheimer's disease (AD).
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文献和实验影响血管紧张素Ⅱ形成的抗高血压药――血管紧张素Ⅰ转化酶抑制剂
普利(ramipril),赖诺普利(lysinopril)及培哚普利(perindopril)等。它们能有效地降低血压,对心功能不全及缺血性心脏病等也有良效。 现代分子生物学研究证明,在心血管、脑、肾等组织中存在着肾素、血管紧张素原的mRNA,局部有相关基因表达,故提出在组织中存在独立的RAAS(系由局部合成),该系统以旁分泌及自分泌方式对心血管及神经系统功能,甚至结构起调节作用。血管中局部产生的血管紧张素Ⅱ(ATⅡ)可增加血管的收缩性能,并促进去甲肾上腺素的释放,而导致血管收缩,血压上升,实验见ATⅡ
oxyphenbutazone perindopril oxytetracycline persantin oxytocics pethidine oxytocin phenacetin phenergan Q
危险降低程度,同时根据具体病人的疾病绝对危险降低程度进行估计(见表6)。 图1 对病人的评估及监测程序 5.2.2.2抗高血压治疗对心血管病危险的绝对效益 l 据国际大量随机化对照的降压临床试验结果,收缩压每降低10~14mmHg或/和舒张压每降低5~6mmHg,脑卒 中危险减少2/5,冠心病减少1/6,总的主要心血管事件减少1/3。据我国4项临床试验的综合分析收缩压每降 低9mmHg或和舒张压每降低4mmHg,脑卒中危险减少36%,冠心病减少3%,总的主要心血管事件减少34%。 l
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