sco792 hydrochloride

Ultrapotent PSEM (uPSEM) agonist for PSAM4-GlyR and PSAM4-5HT3 (Ki = 0.7 nM for PSAM4-GlyR and <10 nM for PSAM4-5HT3). Exhibits >10,000-fold agonist selectivity for PSAM4-GlyR over α7-GlyR, α7-5HT3, and 5HT3-R, and 230-fold selectivity over α4β2 nAChR. Also weak partial agonist (~10 %) at α4β2 nAChR. Retains the potency of varenicline (Cat.No. 3754) for PSAM4-GlyR with enhanced chemogenetic selectivity. Does not act as a substrate for P-glycoprotein pumps. Silences neurons in vivo. Brain-penetrant. Magnus et al (2019) Ultrapotent chemogenetics for research and potential clinical applications. Science doi: 10.1126/science PMID:30872534

SCO-792 is a potent, reversible, orally active inhibitor of enteropeptidase, which slowly dissociates from enteropeptidase in vitro and inhibits protein digestion in vivo.SCO-792 can be used to study the biological effects of enteropeptidase inhibition.

KDI-792 hydrochloride is a thromboxane dual blocker.

Sucunamostat (SCO-792) hydrochloride is an orally active, reversible inhibitor of enteropeptidase, displaying inhibition constants (IC50) of 4.6 nM for rat enteropeptidase and 5.4 nM for human enteropeptidase. In vitro, it dissociates slowly from enteropeptidase, while in vivo, it hinders protein digestion [1].