AHU-377是中性溶酶的抑制剂，IC50值为5 nM。AHU-377和血管紧张素II AT1受体拮抗剂缬沙坦以1：1的摩尔比组成LCZ696。LCZ696是一种血管紧张素受体中性溶酶抑制剂。它可以降低血压，可能是治疗心力衰竭的新药。AHU-377是一种前药，可以通过将乙酯进行酶解将其转化为活性形式LBQ657。据报道，AHU-377（30和100 mg / kg，PO）可以在Dahl-SS大鼠中以剂量依赖的方式引起降压作用。但是在DOCA盐高血压大鼠中，它显示出微弱的降低。 AHU-377 is an inhibitor of neprilysin with IC50 value of 5 nM. AHU-377 and the angiotensin II AT1 receptor antagonist valsartan compose LCZ696 in a 1:1 molar ratio. LCZ696 is an angiotensin receptor neprilysin inhibitor. It can reduce blood pressure and may be a novel drug for the treatment of heart failure. AHU-377 is a prodrug, it can be converted by enzymatic cleavage of the ethyl ester into the active form LBQ657. It is reported that AHU-377(30 and 100 mg/kg, PO) can cause antihypertensive effect in a dose-dependent manner in Dahl-SS rats. But in the DOCA-salt hypertensive rats, it shows a weak reduction.
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AHU 377
CAS number：149709-62-6 molecular formula：C24H29NO5
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compound introduction
Specs
| Chinese alias | (2R,4S)-4-[(3-羧基-1-丙酰基)氨基]-4-[(对-联苯基)甲基]-2-甲基丁酸乙酯 | 4-[[(2S,4R)-5-乙氧基-4-甲基-5-氧代-1-(4-联苯基)戊烷-2-基]氨基]-4-氧代丁酸 | 4-{[(2S,4R)-1-(4-联苯基)-5-乙氧基-4-甲基-5-氧代-2-戊烷基]氨基}-4-氧代丁酸 | (2R,4S)-5-(联苯-4-基)-4-[(3-羧基丙酰基)氨基]-2-甲基戊酸乙酯 | ||
| English alias | SACUBITRIL [ORANGE BOOK] | AHU 377 | (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester | (2R,4S)-5-Biphenyl-4-yl-4-(3-carboxypropionylamino)-2-methylpentanoic acid ethyl ester | 3-{[(2S,4R)-1-{[1,1'-biphenyl]-4-yl}-5 | ||
| CAS number | 149709-62-6 | molecular formula | C24H29NO5 |
| molecular weight | 411.5 g/mol | Exact mass | - |
| PSA | 92.700 Ų | logp | 3.7 |
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