Chemical Properties
Off-White Solid
Uses
A PDE7 inhibitor that has acceptable selectivity for in vivo studies
Biological Activity
Selective, substrate-competitive inhibitor of phosphodiesterase (PDE) 7 (K i = 180 nM). Displays > 200-fold selectivity over PDE1B, PDE1C, PDE2, PDE3, PDE4A4 and PDE5.
Description
BRL-50481 (433695-36-4) is a potent and selective inhibitor of phosphodiesterase-7 (PDE7), Ki=180 nM.1?Induces apoptosis in chronic lymphocytic leukemia cells which express PDE7B.2?BRL-50481 increases mineralization in osteoblasts differentiated from hMSC.3?Cell permeable.
Definition
ChEBI: BRL-50481 is a C-nitro compound that is benzene substituted by N,N-dimethylaminosulfonyl, methyl and nitro groups at positions 1, 2 and 5, respectively. It is a phosphodiesterase inhibitor selective for the PDE7 subtype (Ki = 180 nM). It has a role as an EC 3.1.4.53 (3',5'-cyclic-AMP phosphodiesterase) inhibitor, a geroprotector and a bone density conservation agent. It is a sulfonamide, a C-nitro compound and a member of toluenes.
Biochem/physiol Actions
BRL 50481 is a potent and selective PDE7 inhibitor (IC50 = 260 nM).
References
1) Smith et al. (2004), 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 1679
2) Zhang et al. (2008), Cyclic nucleotide phosphodiesterase profiling reveals increased expression of phosphodiesterase 7B in chronic lymphocytic leukemia; Proc. Natl. Acad. Sci. USA 105 19532
3) Pekkinen et al. (2008), Effects of phosphodiesterase 7 inhibition by RNA interference on the gene expression and differentiation of human mesenchymal stem cell-derived osteoblasts; Bone 43 84
