FBPase-IN-1 is a powerful inhibitor of Fructose-1,6-bisphosphatase (FBPase), a key enzyme involved in Type 2 diabetes (T2D) research. It exhibits an impressive IC50 value of 0.22 μM. Aside from its potency, FBPase-IN-1 also demonstrates the ability to effectively lower blood glucose levels and improve glucose tolerance. Its mechanism of action involves covalently modifying the C128 site, thereby influencing the N125-S124-S123 allosteric pathway of FBPase, ultimately impacting its catalytic activity [1].

FBPase-IN-1 (compund 3a) (1.5625-200 μM, 48 hours) exhibits a low cytotoxicity with an IC 50 of 75.08 μM [1]. FBPase-IN-1 (0-45 min) inhibits FBPase in a time-dependent manner, with IC 50 decreasing from 0.28 to 0.09 μM, shows FBPase-IN-1 is an irreversible covalent inhibitor of FBPase [1].

FBPase-IN-1 (12 h-fasted ICR mouse, n = 6, male, 25 mg/kg, IP) displays good FBPase inhibitory activity ( IC 50 = 0.22 μM), satisfying glucose-lowering effect in vivo (54% reduction in blood glucose at 25 mg/kg) [1]. FBPase-IN-1 (6 or 7 weeks, ICR mice, n = 6, male, 25 mg/kg, IP for 4 hours, once) reduces blood glucose levels by targeting FBPase and inhibiting the GNG process [1]. Animal Model: ICR mouse (12 h-fasted, n = 6, male) [1] Dosage: 25 mg/kg Administration: IP, once Result: Lowered glucose. Animal Model: ICR mice (6 or 7 weeks, n = 6, male) [1] Dosage: 25 mg/kg Administration: IP, for 4 h, once Result: Reduced blood glucose levels by targeting FBPase and inhibiting the GNG process.