All AbMole products are for research use only, cannot be used for human consumption.
In vitro: LCZ696 is a single molecule that is comprised of molecular moieties of valsartan, an ARB, and AHU377, a neprilysin inhibitor (1:1 ratio). AHU377 is converted by enzymatic cleavage of the ethyl ester into the active neprilysin inhibiting metabolite LBQ657. The inactive NEPi precursor, AHU377, does not inhibit collagen accumulation in fibroblasts nor cardiac myocyte hypertrophy. In cardiac fibroblasts, the active NEPi LBQ657 had no discernible effects. In contrast, LBQ657 modestly inhibits cardiac myocyte hypertrophy.
In vivo: In humans, AHU377 (tmax 0.5-1.1 h) are absorbed quickly. AHU377 is converted rapidly into LBQ657 with its tmax being reached in 1.9-3.5 h. Mean t1/2 values for the biologically active LBQ657 is 9.9-11.1 h. In vehicle-treated dogs, ANF increases urinary sodium excretion from 17.3±3.6 to 199.5±18.4 μequiv/kg/min. This effect is potentiated significantly in animals which receive AHU377. Urinary volume is also potentiated in animals which receive an iv administration of AHU377.
| Molecular Weight | 430.52 |
| Formula | C24H28Ca0.5NO5 |
| CAS Number | 1369773-39-6 |
| Solubility (25°C) | 54 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Neprilysin (NEP) Products |
|---|
| Racecadotril
Racecadotril is a peripheral enkephalinase inhibitor with an IC50 of 4.5 μM.Racecadotril and its active metabolite, Thiorphan, inhibited the activity of purified NEP in the mouse brain with Ki's of 4500 and 6.1 nM.May be used in diarrhea related studies. |
| Phosphoramidon disodium salt
Phosphoramidon disodium salt is a microbial metabolite and an inhibitor of the specific metalloproteases thermolysin, endothelin-converting enzyme (ECE), neutralizing peptidase (NEP) and angiotensin-converting enzyme (ACE), with IC50s of 0.4 μg/mL, 3.5 μM, 0.034 μM and 78 μM, respectively. Phosphoramidon disodium salt also prevented the degradation of amyloid β-peptide and increased Aβ levels in rodents. |
| Sacubitrilat
Sacubitrilat (LBQ-657) is an active metabolite of Sacubitril and an inhibitor of enkephalinase (NEP). |
| Sacubitril
Sacubitril (AHU-377) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril (AHU-377) is a component of the heart failure medicine LCZ696. |
| Thiorphan
Thiorphan was a selective neprilysin inhibitor with an IC50 value of 6.9 nM. Increased bradykinin-induced relaxation of isolated porcine coronary rings with potassium chloride precontraction under hypoxic but very oxygen conditions. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
