Angiotensin-converting enzyme (ACE) indirectly increases blood pressure by causing blood vessels to constrict. ACE does that by converting angiotensin I to angiotensin II, which constricts the vessels. ACE, angiotensin I and angiotensin II are part of the renin-angiotensin system (RAS), which controls blood pressure by regulating the volume of fluids in the body. ACE is secreted in the lungs and kidneys by cells in the endothelium (inner layer) of blood vessels. It has two primary functions: ACE catalyses the conversion of angiotensin I to angiotensin II, a potent vasoconstrictor in a substrate concentration-dependent manner. ACE degrades bradykinin, a potent vasodilator, and other vasoactive peptides. These two actions make ACE inhibition a goal in the treatment of conditions such as high blood pressure, heart failure, diabetic nephropathy, and type 2 diabetes mellitus. Inhibition of ACE (by ACE inhibitors) results in the decreased formation of angiotensin II and decreased metabolism of bradykinin, leading to systematic dilation of the arteries and veins and a decrease in arterial blood pressure.
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MLN-4760 (MLN4760) is a potent, selective inhibitor of angiotensin-converting enzyme (ACE)-related carboxypeptidase ACE2 with IC50 of 0.44 nM (hACE2); displays >5,000-fold selectivity over related enzymes including human testicular ACE (IC50>100 uM) and bovine carboxypeptidase A (IC50=27 uM); exacerbated the Ang II-dependent formation of ROS and abolished the generation of Ang-(1-7) from Ang II; exacerbates cardiac hypertrophy and fibrosis in Ren-2 hypertensive rats.
Sampatrilat (UK-81252) is a potent and orally active vasopeptidase inhibitor of ACE and neutral endopeptidase (NEP),Sampatrilat inhibits C-domain ACE (Ki=13.8 nM) 12.4-fold more potent than that for the N-domain (Ki=171.9 nM). Sampatrilat (UK-81252) can be used for the study of chronic heart failure and blood pressure regulation.
Gemopatrilat is a potent, orally available, dual ACE-neutral endopeptidase (vasopeptidase) inhibitor with IC50 of 12 and 63 nM, respectively; causes prolonged inhibition of circulating and renal ACE and renal NEP after a single oral dose in atherogenic diet rabbits.
Omapatrilat is a potent, dual inhibitor of the metalloproteases ACE and NEP with Ki of 0.64 nM and 0.45 nM, respectively; shows moderate activity against APP, and low activity against ECE1; causes significant inhibition of plasma ACE and increases plasma renin activity, reduces blood pressure in spontaneously hypertensive rats; orally active.
Ilepatril is a potent, dual ACE-neutral endopeptidase (vasopeptidase) inhibitor with IC50 of 0.053 and 5.0 nM, respectively; displays good in vitro selectivity over a large variety of targets; restores endothelial function by increasing the ratio of NO to O2- concentration and bioavailability of NO, prevents albuminuria and reduces the incidence and severity of glomerulosclerosis and tubulointerstitial damage in vivo.
Lisinopril is a angiotensin-converting enzyme (ACE) inhibitor for treatment of hypertension, heart failure, and after heart attacks.
Lisinopril dihydrate is a angiotensin-converting enzyme (ACE) inhibitor for treatment of hypertension, heart failure, and after heart attacks.
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