BRL 50481

BRL 50481 is a potent, selective inhibitor of phosphodiesterase (PDE) 7, inhibiting human recombinant PDE7A1 with a K_i value of 180 nM.¹ It is much less effective against PDE3 and PDE4 and is without effect against PDE1B, PDE1C, PDE2, and PDE5.¹ Through its effects on PDE7A1, BRL 50481 enhances the inhibitory effects of the PDE4 blocker rolipram (Item No. 10011132) on monocytes, lung macrophages, and CD8⁺ T-lymphocytes.¹ BRL 50481, at 30 µM, promotes apoptosis in chronic lymphocytic leukemia cells overexpressing PDE7B, suggesting that this compound also acts against PDE7B.² BRL 50481 can be used to evaluate the role of PDE7 isoforms in intracellular signaling.³

WARNING This product is not for human or veterinary use.

1. Smith, S.J., Cieslinski, L.B., Newton, R., et al. 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. Mol. Pharmacol. 66(6), 1679-1689 (2004).

2. Zhang, L., Murray, F., Zahno, A., et al. Cyclic nucleotide phosphodiesterase profiling reveals increased expression of phosphodiesterase 7B in chronic lymphocytic leukemia. Proc. Natl. Acad. Sci. USA 105(49), 19532-19537 (2008).

3. Zhai, K., Hubert, F., Nicolas, V., et al. β-Adrenergic cAMP signals are predominantly regulated by phosphodiesterase type 4 in cultured adult rat aortic smooth muscle cells. PLoS One 7(10), 1-13 (2012).