PF-07976016 (GIPR antagonist 4) is an orally active GIPR antagonist with an IC50 of 4.1 nM. PF-07976016 (GIPR antagonist 4) exerts its antagonistic effect by competitively binding to GIPR and blocking the increase in Gαs -mediated cAMP production induced by GIP agonists. The combination of GIPR antagonist 4 and Liraglutide can enhance the weight loss effect of the single drug. PF-07976016 (GIPR antagonist 4) can be used for research related to obesity and metabolic diseases [1].
In Vivo, In hGIPR KI mice fed a high-fat diet, GIPR antagonist 4 (30 mg/kg; oral; once daily; for 20 days) showed better weight loss in combination with Liraglutide (0.05 mg/kg; subcutaneous injection; once daily; for 20 days) than the single drug group[1].
In Vitro, PF-07976016 (GIPR antagonist 4) (0.1-40 μM; 2.5 h) showed GIPR antagonistic activity in CHO-K1 cells stably expressing the human GIPR receptor, with an IC50 of 4.1 nM.
References:
[1]. Dullea RG, et al. Combination therapy using glucose-dependent insulinotropic polypeptide receptor antagonist compounds and GLP-1 receptor agonist compounds. US20250235460 A1. July 24, 2025.
In Vivo, In hGIPR KI mice fed a high-fat diet, GIPR antagonist 4 (30 mg/kg; oral; once daily; for 20 days) showed better weight loss in combination with Liraglutide (0.05 mg/kg; subcutaneous injection; once daily; for 20 days) than the single drug group[1].
In Vitro, PF-07976016 (GIPR antagonist 4) (0.1-40 μM; 2.5 h) showed GIPR antagonistic activity in CHO-K1 cells stably expressing the human GIPR receptor, with an IC50 of 4.1 nM.
References:
[1]. Dullea RG, et al. Combination therapy using glucose-dependent insulinotropic polypeptide receptor antagonist compounds and GLP-1 receptor agonist compounds. US20250235460 A1. July 24, 2025.