Bropirimine

Bropirimine (U-54461; U-54461S; PNU-54461) is an orally active TLR7 agonist. Bropirimine inhibits RANKL-induced osteoclast differentiation of mouse bone marrow-derived macrophages (BMMs). Bropirimine exhibits dose-dependent direct inhibitory effects on colony formation of cultured KK-47 and 724 cells. Bropirimine can be used for the study of cancers and bone metabolic disorders such as osteoporosis^[1][2][3]. In Vitro:Bropirimine (0.3-30 μg/mL, 3 d) inhibits RANKL-induced osteoclast differentiation of mouse BMMs in a concentration-dependent manner^[1].
Bropirimine (0.3-30 μg/mL, 3 d) suppresses the formation of resorption pits on dentin disks in mouse BMM cultures with RANKL and M-CSF, and significantly reduces mRNA expression of TRAP and NFATc1^[1].
Bropirimine (1-30 μg/mL, 4 d) inhibits 1α,25(OH)2D3-induced osteoclast differentiation of mouse BMCs in co-cultures with mouse osteoblastic UAMS-32 cells in a concentration-dependent manner^[1].
Bropirimine (1-30 μg/mL, 48 h) significantly suppresses 1α,25(OH)2D3-induced RANKL mRNA expression in mouse osteoblastic UAMS-32 cells^[1].
In Vivo:Bropirimine (100-2000 mg/kg, p.o., once daily, 5 consecutive days, starting on day 1 post-tumor inoculation) demonstrates significant anti-tumor efficacy against murine renal-cell carcinoma (Renca) in euthymic BALB/c mice^[3].