BRL-50481

BRL-50481
Clinical data
ATC code
  • None
Identifiers
IUPAC name
  • N,N,2-Trimethyl-5-nitrobenzenesulfonamide
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC9H12N2O4S
Molar mass244.27 g·mol−1
3D model (JSmol)
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 ☒N
  • Key:IFIUFCJFLGCQPH-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

BRL-50481 is a drug developed by GlaxoSmithKline which is the first compound that acts as a phosphodiesterase inhibitor selective for the PDE7 family.[1] PDE7 activity is encoded by two genes, PDE7A and PDE7B. BRL-50481 actually shows about an 80-fold preference for the PDE7A subtype, for which it was developed, over PDE7B.[2] BRL-50481 has been shown to increase mineralisation activity in osteoblasts, suggesting a potential role for PDE7 inhibitors in the treatment of osteoporosis.[3]

References

  1. ↑ Smith SJ, Cieslinski LB, Newton R, Donnelly LE, Fenwick PS, Nicholson AG, et al. (December 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" (PDF). Molecular Pharmacology. 66 (6): 1679–89. doi:10.1124/mol.104.002246. PMID 15371556. S2CID 9491524.
  2. ↑ Alaamery MA, Wyman AR, Ivey FD, Allain C, Demirbas D, Wang L, et al. (April 2010). "New classes of PDE7 inhibitors identified by a fission yeast-based HTS". Journal of Biomolecular Screening. 15 (4): 359–67. doi:10.1177/1087057110362100. PMC 2854023. PMID 20228279.
  3. ↑ Pekkinen M, Ahlström ME, Riehle U, Huttunen MM, Lamberg-Allardt CJ (July 2008). "Effects of phosphodiesterase 7 inhibition by RNA interference on the gene expression and differentiation of human mesenchymal stem cell-derived osteoblasts". Bone. 43 (1): 84–91. doi:10.1016/j.bone.2008.02.021. PMID 18420479.
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