产品说明书

Sacubitril hemicalcium salt

Print
Chemical Structure| 1369773-39-6 同义名 : 沙卡布曲 钙盐 ;AHU-377 hemicalcium salt;AHU377 (calcium salt);Sacubitril
CAS号 : 1369773-39-6
货号 : A120485
分子式 : C48H56CaN2O10
纯度 : 98%
分子量 : 861.044
MDL号 : MFCD28137893
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

溶解度 :

DMSO: 120 mg/mL(139.37 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

动物实验配方:
生物活性
描述 Sacubitril (AHU-377) is a single-molecule drug composed of the molecular parts of Valsartan (ARB) and Sacubitril hemicalsalt (neprilysin inhibitor) (1:1 ratio). Sacubitril (AHU-377) is converted by enzymatic cleavage of ethyl ester to LBQ657, an active metabolite that inhibits neprilysin [2]. Sacubitril hemicalcium salt is an inactive NEPi precursor, which does not inhibit collagen accumulation in fibroblasts nor cardiac myocyte hypertrophy. However, the active NEPi LBQ657 slightly reduces cardiac myocyte hypertrophy without affecting cardiac fibroblasts[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.16mL

0.23mL

0.12mL

5.81mL

1.16mL

0.58mL

11.61mL

2.32mL

1.16mL

参考文献

[1]Ksander GM, et al. Dicarboxylic acid dipeptide neutral endopeptidase inhibitors. J Med Chem. 1995 May 12;38(10):1689-700.

[2]Voors AA, et al. The potential role of valsartan + AHU377 ( LCZ696 ) in the treatment of heart failure. Expert Opin Investig Drugs. 2013 Aug;22(8):1041-7.

[3]von Lueder TG, et al. Angiotensin receptor neprilysin inhibitor LCZ696 attenuates cardiac remodeling and dysfunction after myocardial infarction by reducing cardiac fibrosis and hypertrophy. Circ Heart Fail. 2015 Jan;8(1):71-8.