GUB10194 acetate is a fully potent and selective GPR10 agonist with an EC 50 of 15 nM. GUB10194 acetate does not significantly affect body weight or food intake [1].
In Vivo, GUB10194 (1250 nmol/kg; s.c.; twice daily) acetate does not produce significant body weight loss or food intake inhibition in diet-induced obese mice[1].
In Vitro, GUB10194 (30 min) acetate acts as a full, GPR10-selective agonist in Chem-1 cells expressing GPR10 (EC50 = 15 nM), with no activity detected in CHO-K1 cells expressing NPFF2R (EC50 > 5000 nM)[1].
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.
In Vivo, GUB10194 (1250 nmol/kg; s.c.; twice daily) acetate does not produce significant body weight loss or food intake inhibition in diet-induced obese mice[1].
In Vitro, GUB10194 (30 min) acetate acts as a full, GPR10-selective agonist in Chem-1 cells expressing GPR10 (EC50 = 15 nM), with no activity detected in CHO-K1 cells expressing NPFF2R (EC50 > 5000 nM)[1].
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.