Name | AP5 |
Synonyms | AP5 2H-1-Benzopyran-7-propanoic acid, β-cyclopropyl-2-[2-fluoro-4-(2-methoxy-4-pyridinyl)phenyl]-3,4-dihydro-α-methyl-, (αS,βR,2S)- |
CAS | 1623194-37-5 |
Molecular Formula | C28H28FNO4 |
Molar Mass | 461.53 |
Density | 1.262±0.06 g/cm3(Predicted) |
Boling Point | 596.7±50.0 °C(Predicted) |
pKa | 4.63±0.11(Predicted) |
In vitro study | AP5 is a potent and selective GPR40 AgoPAM that demonstrates excellent in vivo efficacy. In the GK rat oral glucose tolerance test (oGTT), oral administration of AP5 1 h before an oral dextrose challenge shows that AP5 significantly reduces blood glucose levels compared to the vehicle. AP5 is determined to be more efficacious in this model, demonstrating maximally efficacious glucose lowering at a plasma concentration of 4.9 μM at 10 mg/kg. |
biological activity | AP5 is a potent and selective GPR40 receptor agonist, AP5 acts on the GPR40 receptor with an EC50 of 0.49±0.28 nM. |
Target | EC50: 0.49±0.28 nM (GPR40 Receptor) |