貨號	規格	價格	上海	北京	武漢	南京
S83848-5mg	≥97%	￥820.00 S83848-5mg ￥820.00 2-3天	0 貨期：2-3天	-	-	-
S83848-10mg	≥97%	￥1450.00 S83848-10mg ￥1450.00 2-3天	0 貨期：2-3天	-	-	-
S83848-25mg	≥97%	￥3100.00 S83848-25mg ￥3100.00 2-3天	0 貨期：2-3天	-	-	-
S83848-50mg	≥97%	￥5580.00 S83848-50mg ￥5580.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

Omapatrilat is a dual inhibitor of the metalloproteases ACE and NEP with Ki values of 0.64 and 0.45 nM, respectively.

產品描述：

Omapatrilat is a dual inhibitor of the metalloproteases ACE and NEP with Ki values of 0.64 and 0.45 nM, respectively.

靶點：

Ki: 0.45 nM (NEP), 0.64 nM (ACE); IC50: 8 nM (NEP), 5 nM (ACE);RAAS

體內研究：

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

參考文獻：

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.

溶解性：

Soluble in DMSO

保存條件：

2-8℃

配置溶液濃度參考：

	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

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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OMAPATRILAT