TUG-2304 is a highly selective free fatty acid receptor 2 ( FFA2, GPR43 ) antagonist that completely suppresses propionate-induced neutrophil migration and respiratory burst. TUG-2304 is applicable to research related to metabolic and inflammatory diseases [1].
In Vivo, TUG-2304 (compound 16l) (5-10 mg/kg; i.v., p.o.; single dose) exhibits favorable pharmacokinetic properties in male BALB/cAnC mice, with an oral bioavailability of 44%[1].
In Vitro, TUG-2304 (compound 16l) (1 nM-10 μM) completely inhibits propionate-induced migration of human neutrophils over the concentration range of 1 nM to 10 μM[1]. TUG-2304 (100 pM-10 μM) completely inhibits propionate-induced respiratory burst in human neutrophils, with a pIC50 of 8.24 nM, and its activity is specific to FFA2-mediated activation[1].
References:
[1]. Valentini A, et al. Discovery of Potent Tetrazole Free Fatty Acid Receptor 2 Antagonists. Journal of medicinal chemistry. 2023 May 11;66(9):6105-6121.
In Vivo, TUG-2304 (compound 16l) (5-10 mg/kg; i.v., p.o.; single dose) exhibits favorable pharmacokinetic properties in male BALB/cAnC mice, with an oral bioavailability of 44%[1].
In Vitro, TUG-2304 (compound 16l) (1 nM-10 μM) completely inhibits propionate-induced migration of human neutrophils over the concentration range of 1 nM to 10 μM[1]. TUG-2304 (100 pM-10 μM) completely inhibits propionate-induced respiratory burst in human neutrophils, with a pIC50 of 8.24 nM, and its activity is specific to FFA2-mediated activation[1].
References:
[1]. Valentini A, et al. Discovery of Potent Tetrazole Free Fatty Acid Receptor 2 Antagonists. Journal of medicinal chemistry. 2023 May 11;66(9):6105-6121.