Enteropeptidase Inhibitor

Sucunamostat (SCO-792) hydrochloride is an orally active and reversible enteropeptidase inhibitor with IC₅₀s of 4.6 nM and 5.4 nM for rat enteropeptidase and human enteropeptidase, respectively. Sucunamostat hydrochloride can slowly dissociate from enteropeptidase in vitro and inhibit protein digestion in vivo.

Sialorphin TFA is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin TFA blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin TFA regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin TFA exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin TFA also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin TFA is also a copper (II) ion-binding ligand. Sialorphin TFA has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease.

Sucunamostat hydrate (SCO-792) is an orally active and reversible enteropeptidase inhibitor with IC₅₀s of 4.6 nM and 5.4 nM for rat enteropeptidase and human enteropeptidase, respectively. Sucunamostat hydrate can slowly dissociate from enteropeptidase in vitro and inhibit protein digestion in vivo.

Sucunamostat (SCO-792 free acid) is an L-aspartic acid enteropeptidase inhibitor.

Sialorphin is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin is also a copper (II) ion-binding ligand. Sialorphin has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease.

CP-69799 is an azahomostatine-containing oligopeptide transition-state analogue inhibitor with a hog renin IC₅₀ of 6e-9 M, human plasma renin IC₅₀ of 3e-7 M and K_i of 0.310 μM, and endothiapepsin K_i of 0.27 μM. CP-69799 binds endothiapepsin’s active site cleft in extended conformation, fills S4 to S3' pockets, displaces native solvent molecules, induces domain rotation, and reduces thermal mobility of endothiapepsin’s flap and helix regions. CP-69799 acts as a transition-state analogue inhibitor of hog renin and human plasma renin. CP-69799 contains a polar lysine residue at the P2' position, with a nitrogen atom replacing the P1' Cα atom of the hydroxyethylene dipeptide isostere. CP-69799 can be used for the research of hypertension.

Human enteropeptidase-IN-2 (compound 1c) is a highly potent enteropeptidase inhibitor. Human enteropeptidase-IN-2 can be used for anti-obesity research.

(S)-Human enteropeptidase-IN-1 (Compound 6c) is an orally active enteropeptidase inhibitor with low systemic exposure (IC₅₀ (initial): 26 nM; IC₅₀ (app): 1.8 nM). (S)-Human enteropeptidase-IN-1 promotes increased fecal protein output and effectively reduces body weight in a diet-induced obese (DIO) rat model. (S)-Human enteropeptidase-IN-1 inhibits enteropeptidase via a reversible covalent mechanism and prolongs the enzyme inactivation time. (S)-Human enteropeptidase-IN-1 can be used in anti-obesity research.

Human enteropeptidase-IN-1 (compound 6b) is a highly potent, orally active and low systemic exposure enteropeptidase inhibitor. Human enteropeptidase-IN-1 boosts the increase in fecal protein output, and exhibits potent body weight loss in diet-induced obese (DIO) rat model. Human enteropeptidase-IN-1 can be used for anti-obesity research.

Human enteropeptidase-IN-3 is an enteropeptidase inhibitor. Human enteropeptidase-IN-3 exhibits enteropeptidase activity and long duration of inhibitory state. Human enteropeptidase-IN-3 can be used for intetinal digestive related diseases research.