Sacubitril-hemicalcium-salt-AHU-377-hemicalcium-salt-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESacubitril hemicalcium saltCat. No.: HY-15407ACAS No.: 1369773-39-6Synonyms: AHU-377 (hemicalcium salt)分式: CHCa.NO分量: 430.52作靶点: Neprilysin作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-

2、20C 1 month溶解性数据体外实验 DMSO : 54 mg/mL (125.43 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3228 mL 11.6139 mL 23.2277 mL5 mM 0.4646 mL 2.3228 mL 4.6455 mL10 mM 0.2323 mL 1.1614 mL 2.3228 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVI

3、TY物活性 Sacubitril hemicalcium salt (AHU-377 hemicalcium salt)是有效的NEP抑制剂，IC50值为5 nM。AHU-377是治疗衰竭药物LCZ696的个组分。IC50 & Target IC50: 5 nM (NEP) 11/2 Master of Small Molecules 您边的抑制剂师www.MedChemE体外研究 Sacubitril (AHU-377) is a single molecule that is comprised of molecular moieties of valsartan, an ARB, and

4、Sacubitril hemicalcium salt, a neprilysin inhibitor (1:1 ratio). Sacubitril (AHU-377) is converted by enzymaticcleavage of the ethyl ester into the active neprilysin inhibiting metabolite LBQ657 2. The inactive NEPiprecursor, Sacubitril hemicalcium salt, does not inhibit collagen accumulation in fib

5、roblasts nor cardiacmyocyte hypertrophy. In cardiac fibroblasts, the active NEPi LBQ657 had no discernible effects. In contrast,LBQ657 modestly inhibits cardiac myocyte hypertrophy 3.体内研究 In humans, Sacubitril (AHU-377)(tmax 0.5-1.1 h) are absorbed quickly. Sacubitril hemicalcium salt isconverted ra

6、pidly into LBQ657 with its tmax being reached in 1.9-3.5 h. Mean t1/2 values for the biologicallyactive LBQ657 is 9.9-11.1 h 2.In vehicle-treated dogs, ANF increases urinary sodium excretion from17.33.6 to 199.518.4 pequivkglmin. This effect is potentiated significantly in animals which receiveSacub

7、itril (AHU-377). Urinary volume is also potentiated in animals which receive an iv administration ofSacubitril (AHU-377) 1.REFERENCES1. 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 v

8、alsartan + AHU377 ( LCZ696 ) in the treatment of heart failure. Expert Opin Investig Drugs. 2013Aug;22(8):1041-7.3. von Lueder TG, et al. Angiotensin receptor neprilysin inhibitor LCZ696 attenuates cardiac remodeling and dysfunction after myocardialinfarction by reducing cardiac fibrosis and hypertrophy. Circ Heart Fail. 2015 Jan;8(1):71-8.McePdfHeightCaution: Product has not been fully validated for medical applicatio