Enalapril maleate (Vasotec), the active metabolite of enalapril, competes with angiotensin I for binding at the angiotensin-converting enzyme, blocking the conversion of angiotensin I to angiotensin II. Inhibition of ACE results in decreased plasma angiotensin II. As angiotensin II is a vasoconstrictor and a negative-feedback mediator for renin activity, lower concentrations result in a decrease in blood pressure and stimulation of baroreceptor reflex mechanisms, which leads to decreased vasopressor activity and to decreased aldosterone secretion. Enalaprilat may also act on kininase II, an enzyme identical to ACE that degrades the vasodilator bradykinin.
| Molecular Weight | 492.52 |
| Formula | C20H28N2O5.C4H4O4 |
| CAS Number | 76095-16-4 |
| Solubility (25°C) | Water ≥ 10 mg/mL DMSO ≥ 60 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.
| Related ACE Products |
|---|
| Abz-Ser-Pro-3-nitro-Tyr
Abz-Ser-Pro-3-nitro-Tyr is the substrate of ACE2 (angiotensin-converting enzyme-2). |
| Temocaprilat
Temocaprilat (Temocapril diacid) is an inhibitor of angiotensin-converting enzyme (ACE). |
| FA-Phe-Phe
FA-Phe-Phe is a furylacryloyl (fa)-amino acid derivative, targeting to Angiotensin-converting Enzyme (ACE). |
| Garcinone B
Garcinone B, a xanthone derivative, is a nature product that could be isolated from the pericarp of Mangosteen. |
| Spirapril hydrochloride
Spirapril (SCH 33844) hydrochloride is a potent angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Spirapril competitively binds to ACE and prevents the conversion of angiotensin I to angiotensin II. Spirapril is an orally active proagent of Spiraprilat and can be used for the research of hypertension, congestive heart failure. |
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