uPSEM792 hydrochloride，5MG，SML2992-5MG，Sigma

Biochem/physiol Actions

Ultrapotent PSEM agonist for chimeric ligand-gated ion channel pores with nAChR α7 LBD L181G/Q139L/Y217F mutant (PSAM4) in vitro and in vivo.
uPSEM792 is a selective and ultrapotent pharmacologically selective effector molecule (uPSEM) agonist for chimeric pharmacologically selective actuator modules (PSAMs) with mutant nAChR α7 ligand-binding domain (LBD) PSML181G/Q139L/Y217F (PSAM4) fused to the ion pore domain (IPD) of ligand-gated ion channels (LGICs), including glycine receptor (PSAM4-GlyR EC50 = 2.3 nM) and 5-HT3 (PSAM4-5-HT3 EC50 = 1.6 nM). uPSEM792 exhibits high PSM4 selectivity (>10,000-fold over α7-GlyR, α7-5HT3, 5HT3; >230-fold over α4β2 nAChR) and sub-nanomolar PSAM4-GlyR affinity (Ki = 0.7 nM).