ACE Inhibitor

Enalapril (MK-421) is an orally active angiotensin-converting enzyme inhibitor. Enalapril blocks the conversion of angiotensin I to angiotensin II, regulates the renin-angiotensin system, reduces preload and afterload, and decreases plasma angiotensin II levels. Enalapril inhibits apoptosis, reduces nitric oxide metabolite levels, stabilizes endothelial cells, enhances endothelial antioxidant defense, scavenges reactive oxygen species (ROS), and alleviates neuronal damage. Enalapril attenuates glutathione depletion, protein/lipid oxidation, tissue damage, and type III collagen immunolabeling in organs of diabetic rats. Enalapril reduces systolic blood pressure and urinary albumin excretion, and delays the progression of diabetic cardiac/renal injury. Enalapril is used in research related to asymptomatic left ventricular dysfunction, congestive heart failure, Alzheimer's disease, diabetes mellitus, acute myocardial infarction, atrial fibrillation, hypertension, cerebral ischemia, chronic heart failure, and single-ventricle physiology.

Enalapril maleate (MK-421 maleate) is an orally active angiotensin-converting enzyme inhibitor. Enalapril maleate blocks the conversion of angiotensin I to angiotensin II, regulates the renin-angiotensin system, reduces preload and afterload, and decreases plasma angiotensin II levels. Enalapril maleate inhibits apoptosis, reduces nitric oxide metabolite levels, stabilizes endothelial cells, enhances endothelial antioxidant defense, scavenges reactive oxygen species (ROS), and alleviates neuronal damage. Enalapril maleate attenuates glutathione depletion, protein/lipid oxidation, tissue damage, and type III collagen immunolabeling in organs of diabetic rats. Enalapril maleate reduces systolic blood pressure and urinary albumin excretion, and delays the progression of diabetic cardiac/renal injury. Enalapril maleate is used in research related to asymptomatic left ventricular dysfunction, congestive heart failure, Alzheimer's disease, diabetes mellitus, acute myocardial infarction, atrial fibrillation, hypertension, cerebral ischemia, chronic heart failure, and single-ventricle physiology.

Pyrrothiogatain is a transcription factor GATA3 inhibitor with an IC₅₀ of 54.7 μM. Pyrrothiogatain inhibits the DNA-binding activity of GATA3 and inhibits the T helper 2 (Th2) cell differentiation and expression of Th2 cytokines. Pyrrothiogatain shows anti-infection effect by inhibiting ACE2 expression. Pyrrothiogatain can be used for the researches of inflammation, immunology, infection and cancer, such as colon cancer and SARS-CoV-2 infection.

Plantainoside D, a phenylethanoid glycosides, is a IKK-β inhibitor with diverse biological activities. Plantainoside D shows inhibitory activity of angiotensin-converting enzyme (ACE) with an IC₅₀ of 2.17 mM. Plantainoside D significantly reduces the release of glutamate from nerve terminals in the cerebral cortex of rats by inhibiting the voltage-dependent calcium channel (VDCCs) and protein kinase C (PKC) signaling cascade. Plantainoside D significantly alleviates cell apoptosis by inhibiting the generation of ROS and the activation of NF-κB. Plantainoside D significantly improves acute lung injury (ALI) induced by sepsis by regulating the Sirt3/NLRP3 signaling pathway. Plantainoside D can be used for the study of neuroprotection, antioxidant, anti-inflammation, antihypertension.

CV 5975 is an orally active angiotensin converting enzyme (ACE) competitive inhibitor with a rabbit lung ACE IC₅₀ of 3.1 nM and K_i values of 2.6 nM. CV 5975 inhibits ACE in plasma, aorta, kidney, and brain, intensifying inhibition with repeated administration. CV 5975 inhibits Angiotensin I (HY-P1032)-induced pressor responses and ileum contraction, and augments bradykinin-induced ileum contraction and depressor responses. CV 5975 reduces blood pressure via ACE-independent mechanisms, with sustained action across multiple hypertensive and normotensive animal models, intensified by repeated dosing or Hydrochlorothiazide (HY-B0252) co-administration. CV 5975 can be used for the research of hypertension.

FPL 66564 is a short-acting angiotensin-converting enzyme (ACE) inhibitor with an IC₅₀ of 5.7 nM against rabbit ACE. FPL 66564 inhibits ACE activity at the functional level and is hydrolyzed in human blood into inactive hydrophilic metabolites. FPL 66564 modulates angiotensin I-induced pressor responses in anesthetized rats, and its effects rapidly return to baseline after cessation of intravenous infusion. FPL 66564 can be used for research on cardiovascular regulation related to critical illness.

Enalapril-d₅ maleate (MK-421 D₅ maleate) is the deuterated-labeled Enalapril maleate (HY-B0331A). Enalapril maleate is an orally active angiotensin-converting enzyme inhibitor. Enalapril maleate blocks the conversion of angiotensin I to angiotensin II, regulates the renin-angiotensin system, reduces preload and afterload, and decreases plasma angiotensin II levels. Enalapril maleate inhibits apoptosis, reduces nitric oxide metabolite levels, stabilizes endothelial cells, enhances endothelial antioxidant defense, scavenges reactive oxygen species (ROS), and alleviates neuronal damage. Enalapril maleate attenuates glutathione depletion, protein/lipid oxidation, tissue damage, and type III collagen immunolabeling in organs of diabetic rats. Enalapril maleate reduces systolic blood pressure and urinary albumin excretion, and delays the progression of diabetic cardiac/renal injury. Enalapril maleate is used in research related to asymptomatic left ventricular dysfunction, congestive heart failure, Alzheimer's disease, diabetes mellitus, acute myocardial infarction, atrial fibrillation, hypertension, cerebral ischemia, chronic heart failure, and single-ventricle physiology.

Enalapril maleate (Standard) (MK-421 maleate (Standard)) is the analytical standard of Enalapril maleate (HY-B0331A). This product is intended for research and analytical applications. Enalapril maleate is an orally active angiotensin-converting enzyme inhibitor. Enalapril maleate blocks the conversion of angiotensin I to angiotensin II, regulates the renin-angiotensin system, reduces preload and afterload, and decreases plasma angiotensin II levels. Enalapril maleate inhibits apoptosis, reduces nitric oxide metabolite levels, stabilizes endothelial cells, enhances endothelial antioxidant defense, scavenges reactive oxygen species (ROS), and alleviates neuronal damage. Enalapril maleate attenuates glutathione depletion, protein/lipid oxidation, tissue damage, and type III collagen immunolabeling in organs of diabetic rats. Enalapril maleate reduces systolic blood pressure and urinary albumin excretion, and delays the progression of diabetic cardiac/renal injury. Enalapril maleate is used in research related to asymptomatic left ventricular dysfunction, congestive heart failure, Alzheimer's disease, diabetes mellitus, acute myocardial infarction, atrial fibrillation, hypertension, cerebral ischemia, chronic heart failure, and single-ventricle physiology.

Imidapril hydrochloride (TA-6366) is an orally active dual inhibitor of angiotensin-converting enzyme (ACE) and MMP-9. Imidapril hydrochloride inhibits lipopolysaccharide-induced phosphorylation of c-Jun, MKK4 and JNK in monocytes, and downregulates the production of specific inflammatory factors such as TNF-α and IP-10, thereby exerting anti-inflammatory activity. Imidapril hydrochloride also effectively ameliorates mesangial expansion and reduces urinary albumin excretion by inhibiting angiotensin AngII production, lowering glomerular pressure and oxidative stress, thus delaying disease progression. Imidapril hydrochloride can also directly bind to the active site of MMP-9 to inhibit gelatinase activity, and suppress the enlargement of cerebral aneurysms without altering systemic blood pressure. Imidapril hydrochloride is widely applicable to related studies on autoimmune glomerulonephritis, diabetic nephropathy, cerebral aneurysms and other conditions.

αs1-CN f(143–149) is an orally active casein-derived peptide sequence. αs1-CN f(143–149) exhibits angiotensin-converting enzyme (ACE) inhibitory activity (IC₅₀=6.58 μM) and antihypertensive activity.

Ovotransferrin (328-332) has a protective activity on the blood pressure by inhibiting the Angiotensin-Converting Enzyme (ACE), with the IC₅₀ of 20 μM. Ovotransferrin (328-332) fragment has an activity against Cholinesterase (ChE), implicating in Alzheimer’s diseases.

Enalapril sodium (MK-421 sodium) is an orally active angiotensin-converting enzyme inhibitor. Enalapril sodium blocks the conversion of angiotensin I to angiotensin II, regulates the renin-angiotensin system, reduces preload and afterload, and decreases plasma angiotensin II levels. Enalapril sodium inhibits apoptosis, reduces nitric oxide metabolite levels, stabilizes endothelial cells, enhances endothelial antioxidant defense, scavenges reactive oxygen species (ROS), and alleviates neuronal damage. Enalapril sodium attenuates glutathione depletion, protein/lipid oxidation, tissue damage, and type III collagen immunolabeling in organs of diabetic rats. Enalapril sodium reduces systolic blood pressure and urinary albumin excretion, and delays the progression of diabetic cardiac/renal injury. Enalapril sodium is used in research related to asymptomatic left ventricular dysfunction, congestive heart failure, Alzheimer's disease, diabetes mellitus, acute myocardial infarction, atrial fibrillation, hypertension, cerebral ischemia, chronic heart failure, and single-ventricle physiology.

RB-105 is an inhibitor of angiotensin-converting enzyme (ACE) (K_i = 4.2 nM) and neutral endopeptidase (NEP) (K_i = 1.7 nM). RB-105 after inhibiting ACE reduces the production of Ang II and increase the level of bradykinin. RB-105 after inhibiting NEP increases the level of natriuretic peptide and further increases the level of bradykinin, thereby generating a powerful synergistic effect. RB-105 has significant antihypertensive and natriuretic effects in both spontaneously hypertensive rats and normal blood pressure rats. RB-105 can be used for research on hypertension.

Gemopatrilat (BMS-189921) is an orally active vasopeptidase inhibitor with IC₅₀ value of 12 nM. Gemopatrilat can be used in studies of hypertension and congestive heart failure.

Enalapril-d₃ (MK-421-d₃) is the deuterated-labeled Enalapril (HY-B0331). Enalapril is an orally active angiotensin-converting enzyme inhibitor. Enalapril blocks the conversion of angiotensin I to angiotensin II, regulates the renin-angiotensin system, reduces preload and afterload, and decreases plasma angiotensin II levels. Enalapril inhibits apoptosis, reduces nitric oxide metabolite levels, stabilizes endothelial cells, enhances endothelial antioxidant defense, scavenges reactive oxygen species (ROS), and alleviates neuronal damage. Enalapril attenuates glutathione depletion, protein/lipid oxidation, tissue damage, and type III collagen immunolabeling in organs of diabetic rats. Enalapril reduces systolic blood pressure and urinary albumin excretion, and delays the progression of diabetic cardiac/renal injury. Enalapril is used in research related to asymptomatic left ventricular dysfunction, congestive heart failure, Alzheimer's disease, diabetes mellitus, acute myocardial infarction, atrial fibrillation, hypertension, cerebral ischemia, chronic heart failure, and single-ventricle physiology.

SARS-CoV-2-IN-116 (Compound (S,S)-4) is a highly selective angiotensin-converting enzyme 2 (ACE2) inhibitor (pIC₅₀=7.61). SARS-CoV-2-IN-116 blocks the interaction between SARS-CoV-2 spike protein and ACE2. SARS-CoV-2-IN-116 is promising for research of COVID-19.