LBQ657 is an active metabolite of Sacubitril and an inhibitor of enkephalinase (NEP).
| Molecular Weight | 383.44 |
| Formula | C22H25NO5 |
| CAS Number | 149709-44-4 |
| Solubility (25°C) | DMSO >100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[3] Scott A Hubers, et al. Combined Angiotensin Receptor Antagonism and Neprilysin Inhibition
| Related Neprilysin (NEP) Products |
|---|
| Opiorphin
Opiorphin is an opioid peptide that simultaneously inhibits the activity of two enkephalinolytic enzymes, human neutral exopeptide endogenous peptidase hNEP (EC 3.4.24.11) and human exoamino peptidase hAP-N (EC 3.4.11.2). |
| 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. |
| 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. |
| Omapatrilat
Omapatrilat is a vasopeptidase inhibitor, a dual metalloprotease inhibitor of neutral endopeptidase (NEP, neprilysin) and angiotensin converting enzyme (ACE). |
| 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. |
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