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.
| Molecular Weight | 385.48 |
| Formula | C21H23NO4S |
| CAS Number | 81110-73-8 |
| Solubility (25°C) | DMSO 20 mg/mL Ethanol 70 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] No authors listed. Drug Ther Bull. What place for ▾racecadotril?
[4] A J Matheson, et al. Racecadotril
[5] J C Schwartz. Racecadotril: a new approach to the treatment of diarrhoea
| 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. |
| LBQ657
LBQ657 is an active metabolite of Sacubitril and an inhibitor of enkephalinase (NEP). |
| Omapatrilat
Omapatrilat is a vasopeptidase inhibitor, a dual metalloprotease inhibitor of neutral endopeptidase (NEP, neprilysin) and angiotensin converting enzyme (ACE). |
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