GUB08248 acetate is a full GPR10 agonist and a partial NPFF2R agonist, with EC 50 values of 0.5 nM and 2.5 nM, respectively. GUB08248 acetate inhibits food intake and induces sustained weight loss. GUB08248 acetate can be used in obesity-related research [1] [2].
In Vivo, GUB08248 (1250 nmol/kg; s.c.; twice daily) acetate nduces robust, sustained body weight loss of 13.5% relative to baseline and transient food intake suppression in diet-induced obese mice[1].
In Vitro, GUB08248 (30 min) acetate acts as a potent dual full agonist of GPR10 and partial agonist of NPFF2R in Chem-1 cells expressing GPR10 and CHO-K1 cells expressing NPFF2R, with EC50 values of 0.5 nM and 2.5 nM, respectively[1]. GUB08248 (1 h) acetate potently activates wild-type NPFF2R in HEK293T cells[2].
References:
[1]. Alexopoulou F, et al. Lipidated PrRP31 metabolites are long acting dual GPR10 and NPFF2 receptor agonists with potent body weight lowering effect. Sci Rep. 2022;12(1):1696. Published 2022 Feb 1.
[2]. Li X, et al. Molecular basis for cross-activation of NPFF2R by a short PrRP-related peptide. Acta Pharmacol Sin. Published online February 4, 2026.
In Vivo, GUB08248 (1250 nmol/kg; s.c.; twice daily) acetate nduces robust, sustained body weight loss of 13.5% relative to baseline and transient food intake suppression in diet-induced obese mice[1].
In Vitro, GUB08248 (30 min) acetate acts as a potent dual full agonist of GPR10 and partial agonist of NPFF2R in Chem-1 cells expressing GPR10 and CHO-K1 cells expressing NPFF2R, with EC50 values of 0.5 nM and 2.5 nM, respectively[1]. GUB08248 (1 h) acetate potently activates wild-type NPFF2R in HEK293T cells[2].
References:
[1]. Alexopoulou F, et al. Lipidated PrRP31 metabolites are long acting dual GPR10 and NPFF2 receptor agonists with potent body weight lowering effect. Sci Rep. 2022;12(1):1696. Published 2022 Feb 1.
[2]. Li X, et al. Molecular basis for cross-activation of NPFF2R by a short PrRP-related peptide. Acta Pharmacol Sin. Published online February 4, 2026.