JBSNF-000028 TFA, a nicotinamide N-methyltransferase (NNMT) inhibitor, exhibits oral activity with inhibitory concentration 50 (IC50) values of 0.033 μM, 0.19 μM, and 0.21 μM for human NNMT (hNNMT), monkey NNMT (mkNNMT), and mouse NNMT (mNNMT) respectively. It is applicable in metabolic disorder research [1].

JBSNF-000028 TFA, after 24 hours of exposure, effectively suppresses NNMT activity, exhibiting an EC50 value of 2.5 μM in U2OS cells [1]. When tested at concentrations ranging from 10-100 μM for 72 hours, JBSNF-000028 TFA demonstrates no cytotoxic effects on HepG2 cells [1]. The compound specifically interacts with the nicotinamide binding site, inserting itself beneath a hairpin structure and forming stacking interactions between Tyr-204 (from the Hairpin) and Leu-164 (from the central domain) [1]. Additionally, JBSNF-000028 TFA shows inactivity across a comprehensive spectrum of metabolic and safety-related targets [1].

JBSNF-000028 TFA, administered orally at a dose of 50 mg/kg twice daily, enhances glucose and lipid metabolism over 27 days in mice with diet-induced obesity (DIO) [1], and similarly improves glucose tolerance in NNMT knockout mice with DIO when given for 4 weeks [1].