计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
避光,充氩,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Omapatrilat is a dual inhibitor of the metalloproteases ACE and NEP with K i values of 0.64 and 0.45 nM, respectively.
In Vitro
Omapatrilat exhibits high potency for NEP, NEP2 and ACE, moderate strong activity against APP, but low activity against ECE1 (K i =0.45, 25, 0.64, 250 nM). In vitro autoradiography using the specific NEP inhibitor radioligand 125I-RB104 and the specific ACE inhibitor radioligand 125I-MK351A show omapatril at (10 mg/kg) causes rapid and potent inhibition of renal NEP and ACE, respectively, for 24 h . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:Ki: 0.45 nM (NEP), 0.64 nM (ACE), ,\nIC50: 8 nM (NEP), 5 nM (ACE)
规格
别名
奥马曲拉
规格或纯度
10mM in DMSO
英文名称
Omapatrilat
生化机理
Omapatrilat 是金属蛋白酶 ACE 和 NEP 的双重抑制剂，其 K i 值分别为 0.64 和 0.45 nM。
储存条件
避光,充氩,-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
EC号
110-388-4
分子类型
小分子
Isomeric SMILES
C1C[C@H](N2[C@H](C1)SCC[C@@H](C2=O)NC(=O)[C@H](CC3=CC=CC=C3)S)C(=O)O
PubChem CID
分子量
408.53
技术文档
高级数据
关联靶点（人）
MME
Tclin
脑啡肽酶(Neprilysin)
(2 活性数据)
ACE
Tclin
血管紧张素转换酶(Angiotensin-converting enzyme)
(6 活性数据)
APP
Tclin
淀粉样β蛋白A4(Amyloid-beta A4 protein)
(1 活性数据)
安全和危险性（GHS）
RIDADR
NONHforallmodesoftransport
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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