Sacubitril-13C4 (AHU-377-13C4) hemicalcium salt 是 13C 和氘代标记的 Sacubitril hemicalcium salt。Sacubitril (AHU-377) hemicalcium salt 是有效的NEP抑制剂，IC50值为5 nM。Sacubitril hemicalcium salt 是研究心力衰竭药物 LCZ696 的一个组分。
Sacubitril-13C4 (AHU-377-13C4) hemicalcium salt is a 13C-labeled and deuterium labeled Sacubitril hemicalcium salt. Sacubitril (AHU-377) hemicalcium salt is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril hemicalcium salt is a component of the heart failure medicine LCZ696[1].
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Ksander GM, et al. Dicarboxylic acid dipeptide neutral endopeptidase inhibitors. J Med Chem. 1995 May 12;38(10):1689-700.;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.;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.
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