Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Omapatrilat is a metalloprotease ACE and NEP dual inhibitor (Ki: 0.64 and 0.45 nM, respectively).
产品描述 | Omapatrilat is a metalloprotease ACE and NEP dual inhibitor (Ki: 0.64 and 0.45 nM, respectively). |
靶点活性 | ACE:0.64 nM(ki), NEP:(ki)0.45 nM |
体外活性 | In vitro autoradiography using the specific NEP inhibitor radioligand 125I-RB104 and the specific ACE inhibitor radioligand 125I-MK351A display omapatril at (10 mg/kg) induces rapid and effective inhibition of renal NEP and ACE, respectively, for 24 h. Omapatrilat displays high potency for NEP, NEP2 and ACE, moderate strong activity against APP, but low activity against ECE1 (Ki=0.45, 25, 0.64, 250 nM) [1][4]. |
体内活性 | Omapatrilat is widely used in experimental protocols related to hypertension and heart failure. Omapatrilat reduces mean arterial pressure (MAP) approximately 40 mmHg below baseline from 10 to 24 h. Omapatrilat shows 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 (p.o.; 100 μM/kg; once daily) causes a 38 mmHg decrease in systolic blood pressure at day three as compared to the vehicle [2]. Omapatrilat(Chronic oral administration) decreases aortic leakiness and atheroma formation with enhanced endothelial independent vasorelaxation to ANP[3]. Omapatrilat leads to significant inhibition of plasma ACE and increased plasma renin activity in rats[4]. |
别名 | BMS-186716 |
分子量 | 408.53 |
分子式 | C19H24N2O4S2 |
CAS No. | 167305-00-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 31 mg/mL (75.88 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4478 mL | 12.239 mL | 24.478 mL | 61.195 mL |
5 mM | 0.4896 mL | 2.4478 mL | 4.8956 mL | 12.239 mL | |
10 mM | 0.2448 mL | 1.2239 mL | 2.4478 mL | 6.1195 mL | |
20 mM | 0.1224 mL | 0.612 mL | 1.2239 mL | 3.0598 mL | |
50 mM | 0.049 mL | 0.2448 mL | 0.4896 mL | 1.2239 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Omapatrilat 167305-00-2 Endocrinology/Hormones RAAS BMS 186716 BMS186716 BMS-186716 Inhibitor inhibitor inhibit