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产品描述： Omapatrilat is a dual inhibitor of the metalloproteases ACE and NEP with Ki values of 0.64 and 0.45 nM, respectively. |
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靶点：
Ki: 0.45 nM (NEP), 0.64 nM (ACE); IC50: 8 nM (NEP), 5 nM (ACE);RAAS |
体内研究：
Omapatrilat demonstrates excellent blood pressure lowering in a variety of animal models characterized by various levels of plasma renin activity and significantly potentiates urinary sodium, ANP, and cGMP excretion in a cynomolgus monkey assay. Omapatrilat decreases mean arterial pressure (MAP) approximately 40 mmHg below baseline from 10 to 24 h. Oral administration of omapatrilat at 100 μM/kg once daily results in a 38 mmHg decrease in systolic blood pressure at day three as compared to vehicle. Omapatrilat is widely used in experimental protocols related to hypertension and heart failure. Chronic oral administration of omapatrilat reduces aortic leakiness and atheroma formation with enhanced endothelial independent vasorelaxation to ANP. Omapatrilat causes significant inhibition of plasma ACE and increased plasma renin activity in rats |
参考文献：
1. Fryer RM, et al. Effect of bradykinin metabolism inhibitors on evoked hypotension in rats: rank efficacy ofenzymes associated with bradykinin-mediated angioedema.Br J Pharmacol. 2008 Mar;153(5):947-55. 2. Robl JA, et al. Dual metalloprotease inhibitors: mercaptoacetyl-based fused heterocyclic dipeptide mimetics asinhibitors of angiotensin-converting enzyme and neutral endopeptidase. J Med Chem. 1997 May 23;40(11):1570-7. 3. Ichiki T, et al. Endothelial permeability in vitro and in vivo: protective actions of ANP and omapatrilat in experimental atherosclerosis. Peptides. 2013 Oct;48:21-6. 4. Burrell LM, et al. Antihypertensive and antihypertrophic effects of omapatrilat in SHR. Am J Hypertens. 2000 Oct;13(10):1110-6. |
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溶解性：
Soluble in DMSO |
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保存条件：
2-8℃ |
配置溶液浓度参考：
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1mg |
5mg |
10mg |
| 1 mM |
2.448 ml |
12.239 ml |
24.478 ml |
| 5 mM |
0.49 ml |
2.448 ml |
4.896 ml |
| 10 mM |
0.245 ml |
1.224 ml |
2.448 ml |
| 50 mM |
0.049 ml |
0.245 ml |
0.49 ml |
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| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
北京