Anti-osteoporosis agent-8 (Compound 4aa) is a RANKL inhibitor, capable of preventing RANKL-induced osteoclastogenesis and osteoclast differentiation, with an IC50 of 2.41 μM. Furthermore, Anti-osteoporosis agent-8 has been shown to mitigate bone loss in an ovariectomized (OVX) mouse model.

Anti-osteoporosis agent-8 promotes osteoblast differentiation in MC3T3-E1 cells by activating the BMP2 signaling pathway at concentrations of 0-10 μM over 5 days. Additionally, at a concentration of 5 μM for 6 hours, it inhibits the expression of osteoclast-related genes, osteoclastogenesis, and osteoclast bone resorption by suppressing the MAPK and NF-κB signaling pathways.

An anti-osteoporosis agent-8, administered at a dosage of 10 mg/kg via intraperitoneal injection every two days for a duration of eight weeks, effectively prevents bone loss caused by ovariectomy in the C57BL/6 mouse model.