TN-783 is an orally active, brain-penetrant NLRP3 ( IC50 = 19.3 nM) inhibitor. TN-783 enhances the effects of the GLP-1 receptor agonist semaglutide. TN-783 requires sustained targeted action, not permanent metabolic remodeling. TN-783 can be used for the study of obesity [1].
In Vivo, TN-783 (0.5-50 mg/kg, p.o., twice daily, 14-66 days) can achieve safe (lean body mass preservation), effective, and reversible weight loss by reducing hypothalamic neuroinflammation[1].
In Vitro, TN-783 (2 h) can effectively inhibit the secretion of IL-1β (IC50 = 45.9 nM) by THP-1 cells, under Lipopolysaccharides (LPS)/Nigericin stimulation[1]. TN-783 (0.3 nM-6 μM, 1 h) can dose-dependently inhibit the secretion of IL-1β (IC50 = 5.17 nM) and IL-18 (IC50 = 12.3 nM) in THP-1 cells induced by Palmitic acid -BSA complex[1].
In Vivo, TN-783 (0.5-50 mg/kg, p.o., twice daily, 14-66 days) can achieve safe (lean body mass preservation), effective, and reversible weight loss by reducing hypothalamic neuroinflammation[1].
In Vitro, TN-783 (2 h) can effectively inhibit the secretion of IL-1β (IC50 = 45.9 nM) by THP-1 cells, under Lipopolysaccharides (LPS)/Nigericin stimulation[1]. TN-783 (0.3 nM-6 μM, 1 h) can dose-dependently inhibit the secretion of IL-1β (IC50 = 5.17 nM) and IL-18 (IC50 = 12.3 nM) in THP-1 cells induced by Palmitic acid -BSA complex[1].