产品说明书
Sacubitril
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同义名 : | AHU-377 |
| CAS号 : | 149709-62-6 | |
| 货号 : | A269433 | |
| 分子式 : | C24H29NO5 | |
| 纯度 : | 98% | |
| 分子量 : | 411.491 | |
| MDL号 : | MFCD00920862 | |
| 存储条件： |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 80 mg/mL(194.42 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | AHU-377 is a Neprilysin inhibitors (NEPi) with an IC50 of 5 nM[3].It prevents the degradation of natriuretic peptides and activate cGMP signalling pathways that regulate volume and blood pressure. In normotensive rats, pretreatment with AHU-377 (3, 10 and 30 mg/kg, PO.) augmented ANP-evoked (atrial natriuretic peptide) plasma cGMP levels by 2.4, 3.3 and 4.0 fold, respectively (4h AUC compared to vehicle). In Dahl-SS (Dahl-salt-sensitive) rats, AHU-377 (30 and 100 mg/kg, PO) produced a dose-dependent antihypertensive effect. AHU-377 enhances the tone of the natriuretic peptide system and exerts significant antihypertensive effects[4]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT01601470 | Mild to Moderate Hypertension | Phase 2 | Completed | - | Germany ... 展开 >> Novartis Investigative Site Berlin, Germany, 14050 收起 << |
| NCT01569815 | Mild and Moderate Renal Impair... 展开 >>ment 收起 << | Phase 1 | Completed | - | Germany ... 展开 >> Novartis Investigative Site Neuss, Germany, 41460 Russian Federation Novartis Investigative Site Moscow, Russian Federation, 117292 Serbia Novartis Investigative Site Belgrade, Serbia 收起 << |
| NCT01621633 | Hepatic Impairment | Phase 2 | Completed | - | Germany ... 展开 >> Novartis Investigative Site Grunstadt, Germany, D-67269 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.43mL 0.49mL 0.24mL |
12.15mL 2.43mL 1.22mL |
24.30mL 4.86mL 2.43mL |
| 参考文献 |
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