Angiotensin-converting Enzyme (ACE) Inhibitor

Ursodeoxycholic acid (Ursodeoxycholate) is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Ursodeoxycholic acid also reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection. Orally active.

Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC₅₀=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC₅₀ of 7.9 μM.

Angiotensin 1-7 (Ang-(1-7)) is an endogenous heptapeptide from the renin-angiotensin system (RAS) with a cardioprotective role due to its anti-inflammatory and anti-fibrotic activities in cardiac cells. Angiotensin 1-7 inhibits purified canine ACE activity (IC₅₀=0.65 μM). Angiotensin 1-7 acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium. Angiotensin 1-7 shows anti-inflammatory activity .

HD5 TFA is an innate immune effector peptide and SARS-CoV Inhibitor. HD5 TFA binds to the ligand-binding domain of angiotensin-converting enzyme-2 (ACE2) via multiple hydrogen bonds to competitively block the receptor, shielding it from viral recognition. HD5 TFA can be used for the research of COVID-19, HPV16 infection, epithelial ovarian cancer, small-cell lung cancer, and colon cancer.

VYPFPGPIHN is a precursor peptide of β-casomorphin (HY-P0179) and also an ACE inhibitor (IC₅₀ = 123 μM). VYPFPGPIHN resists hydrolysis by peptidases associated with intestinal cell monolayers, maintaining structural integrity and ACE inhibitory activity. VYPFPGPIHN is not extensively taken up or transported by differentiated intestinal cell monolayers.

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.

Lisinopril (MK-521) is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.

Enalapril (MK-421) is an angiotensin-converting enzyme (ACE) inhibitor, can be used for hypertensive diseases research.

Enalapril (MK-421) maleate, the active metabolite of enalapril, is an angiotensin-converting enzyme (ACE) inhibitor.

MLN-4760 is a potent and selective human ACE2 inhibitor (IC₅₀, 0.44 nM), with excellent selectivity (>5000-fold) versus related enzymes including human testicular ACE (IC₅₀, >100 μM) and bovine carboxypeptidase A (CPDA; IC₅₀, 27 μM).

(Z)-Guggulsterone, a constituent of Indian Ayurvedic medicinal plant Commiphora mukul, inhibits the growth of human prostate cancer cells by causing apoptosis. (Z)-Guggulsterone inhibits angiogenesis by suppressing the VEGF–VEGF-R2–Akt signaling axis. (Z)-Guggulsterone is also a potent FXR antagonist. (Z)-Guggulsterone reduces ACE2 expression and SARS-CoV-2 infection.

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.

Sinapinic acid (Sinapic acid) is a phenolic compound isolated from Hydnophytum formicarum Jack. Rhizome, acts as an inhibitor of HDAC, with an IC₅₀ of 2.27 mM, and also inhibits ACE-I activity. Sinapinic acid posssess potent anti-tumor activity, induces apoptosis of tumor cells. Sinapinic acid shows antioxidant and antidiabetic activities. Sinapinic acid reduces total cholesterol, triglyceride, and HOMA-IR index, and also normalizes some serum parameters of antioxidative abilities and oxidative damage in ovariectomized rats.

Ramipril (HOE-498) is an angiotensin-converting enzyme (ACE) inhibitor with IC₅₀ of 5 nM.

Lisinopri dihydrate (MK-521 dihydrate) is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.

Perindopril erbumine is an angiotensin-converting enzyme inhibitor. Perindopril erbumine modulates NFκB and STAT3 signaling and inhibits glial activation and neuroinflammation. Perindopril erbumine can be used for the research of Chronic Kidney Disease and high blood pressure.

BMS-265246 is a potent and selective cyclin-dependent kinase CDK1 and CDK2 inhibitor, with IC₅₀ values of 6 and 9 nM, respectively. BMS-265246 inhibits CHI3L1 (chitinase 3-like-1) stimulation of ACE2 (angiotensin converting enzyme 2) and SPP (viral spike protein priming proteases). BMS-265246 can be used for ovarian cancer and COVID-19 research.

Alamandine, a member of the renin-angiotensin system (RAS), a vasoactive peptide, is an endogenous ligand of the G protein-coupled receptor MrgD. Alamandine targets to protect the kidney and heart through anti-hypertensive actions.

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.

Phosphoramidon disodium, a microbial metabolite, is a specific metalloprotease thermolysin inhibitor with an IC₅₀ of 0.4 μg/mL. Phosphoramidon disodium also inhibits endothelin-converting enzyme (ECE), neutral endopeptidase (NEP), and angiotensin-converting enzyme (ACE) with IC₅₀ values of 3.5, 0.034, and 78 μM, respectively.