Adhesion G Protein-coupled Receptors (AGPCRs) Agonist

AP-503 is a selective GPR133/ADGRD1 agonist with an EC₅₀ of 1.21 nM. AP-503 is used in research on the prevention of muscle-related diseases and vestibular dysfunction.

Vmm-p15 is a peptide agonist optimized for the adhesion G protein-coupled receptor GPR64 (also known as ADGRG2 or HE6). The affinity of VPM-p15 with GPR64 is significantly higher than that of the original p15 peptide. The cAMP level induced by VMM-P15 increased significantly, activated GPR64, and triggered downstream Gs, Gq, and G12/13 signaling. VPM-p15 can be used to study the activation mechanism of adherent GPCR family members.

GPR133 agonist 1 is an orally active GPR133/ADGRD1 agonist with an EC₅₀ of 1.6 nM (293T cells). GPR133 agonist 1 activates GPR133, thereby regulating the downstream cAMP signaling pathway. GPR133 agonist 1 enhances muscle strength and endurance in mice. GPR133 agonist 1 can be used in research related to muscular atrophy, myasthenia, sarcopenia, erectile dysfunction, vestibular dysfunction, obesity, and non-alcoholic fatty liver disease.

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 (HY-P0014) 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.

(3aS,4R,9bR)-G-1 is a highly selective G protein-coupled receptor GPR30 (GPER) agonist with a K_i value of approximately 7 nM. (3aS,4R,9bR)-G-1 activates rapid signaling pathways such as intracellular calcium mobilization and PI3K signaling through GPR30, promoting uterine epithelial cell proliferation and exerting antidepressant effects. (3aS,4R,9bR)-G-1 is promising for research of breast cancer and depression.