BI-9508

BI-9508, a compound developed through medicinal chemistry modification based on existing scaffold, has proven to be a promising active compound, demonstrating significant progress in both in vitro and in vivo activities. Notably, BI-9508 exhibits high selectivity at the cellular level, allowing it to effectively and selectively bind to the target receptor GPR88, thereby contributing to the regulation of nervous system functions. In in vivo studies, BI-9508 has shown robust pharmacological efficacy, particularly in C57BL6/N mice, following both oral administration and intraperitoneal injection. Additionally, its pharmacokinetic properties have improved. However, the compound does have some limitations, such as its high lipophilicity, which may impact its distribution and efficacy within biological systems and may also lead to P-glycoprotein (PGP) efflux. Despite these challenges, BI-9508 remains an exceptional choice as a tool compound, well-suited for further research and exploration of GPR88 functions.

BI-9508 appears to be the best available tool compound as a GPR88 agonist (i.e. GPR88 agonistic chemical probe), making it valuable for in vitro studies and structural biology experiments. This compound could also be useful for in vivo studies; however, users should carefully conduct in vivo experiments due to its profiles, such as relatively high lipophilicity and significant plasma protein binding properties, which could significantly impact pharmacokinetic parameters in each experiment. It is recommended to consult with researchers who have expertise in pharmacokinetics before conducting experiments.