Published TCIMAIL newest issue No.197
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Phosphodiesterase 7 Inhibitor
No.177(April 2018)
BRL 50481 (1) is a selective inhibitor of phosphodiesterase 7 (PDE7).1) 1 inhibits human recombinant PDE7 in a competitive manner (Ki = 180 nM). 1 is much less potent against PDE3 and PDE4 (Table 1). In addition, treatment of human mesenchymal stem cell-derived osteoblasts with 1 increased mineralization.2)
Table 1. Selectivity of BRL 50481 (1) to PDE isoenzymes1)
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References
- 1)Discovery of BRL 50481 [3-(N,N-dimethylsulfonamido)-4-methyl-nitrobenzene], a selective inhibitor of phosphodiesterase 7: In vitro studies in human monocytes, lung macrophages, and CD8+ T-lymphocytes
- 2)Effects of phosphodiesterase 7 inhibition by RNA interference on the gene expression and differentiation of human mesenchymal stem cell-derived osteoblasts
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