BRL-50481

BRL-50481

Systematic (IUPAC) name
N,N,2-Trimethyl-5-nitro-benzenesulfonamide
Identifiers
CAS Number	433695-36-4
PubChem	CID 2921148
IUPHAR/BPS	5154
ChemSpider	2194720
ChEMBL	CHEMBL484928
Chemical data
Formula	C9H12N2O4S
Molar mass	244.267 g/mol
SMILES Cc1ccc(N(=O)=O)cc1S(=O)(=O)N(C)C
InChI InChI=1S/C9H12N2O4S/c1-7-4-5-8(11(12)13)6-9(7)16(14,15)10(2)3/h4-6H,1-3H3 Key:IFIUFCJFLGCQPH-UHFFFAOYSA-N
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BRL-50481 is a drug developed by GlaxoSmithKline which is the first compound that acts as a phosphodiesterase inhibitor selective for the PDE₇ subtype.^[1] It has been shown to increase mineralisation activity in osteoblasts, suggesting a potential role for PDE₇ inhibitors in the treatment of osteoporosis.^[2]

References

1. Smith SJ, Cieslinski LB, Newton R, Donnelly LE, Fenwick PS, Nicholson AG, Barnes PJ, Barnette MS, Giembycz MA. 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. Molecular Pharmacology. 2004 Dec;66(6):1679-89. PMID 15371556
2. Pekkinen M, Ahlström ME, Riehle U, Huttunen MM, Lamberg-Allardt CJ. Effects of phosphodiesterase 7 inhibition by RNA interference on the gene expression and differentiation of human mesenchymal stem cell-derived osteoblasts. Bone. 2008 Jul;43(1):84-91. PMID 18420479