Omapatrilat
产品说明书
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同义名 : | BMS-186716 |
| CAS号 : | 167305-00-2 | |
| 货号 : | A410726 | |
| 分子式 : | C19H24N2O4S2 | |
| 纯度 : | 98% | |
| 分子量 : | 408.53 | |
| MDL号 : | N/A | |
| 存储条件： |
Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Omapatrilat was originally identified as a selective dual inhibitor of angiotensin-converting enzyme (ACE) and neprilysin (NEP). The K values of omapatrilat against NEP, NEP2, endothelin-converting enzyme 1 (ECE1), ACE, and aminopeptidase P (APP) were 0.00045, 0.025, 10, 0.00064, and 0.25μM, respectively. In Sprague–Dawley rats subjected to an optimal dose of bradykinin (100ng/min), omapatrilat (0.0, 0.53, 1.76, or 5.3mg/kg) resulted in a dose-dependent reduction in the mean arterial blood pressure area under the curve (MAP AUC). Peak reduction was observed in the group administered with 1.76 and 5.3mg/kg omapatrilat. The effect of omapatrilat on MAP AUC was reduced when the doses of bradykinin decreased (10 and 30ng/min). Rats administered with omapatrilat at doses of 1.76 and 5.3mg/kg exhibited blunted reflex tachycardia.[1] | ||
| 作用机制 | Omapatrilat exhibits potent inhibitory activity against three bradykinin-metabolizing enzymes: NEP, ACE, and APP. The concomitant inhibition of both APP and ACE by omapatrilat is probably the primary mechanism responsible for the large depressor response in rats and angioedema in patients.[1] | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.45mL 0.49mL 0.24mL |
12.24mL 2.45mL 1.22mL |
24.48mL 4.90mL 2.45mL |
| 参考文献 |
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