| Identification | Back Directory | [Name]
BRL 50481 | [CAS]
433695-36-4 | [Synonyms]
BRL 50481
5-NITRO-2,N,N-TRIMETHYLBENZENESULFONAMIDE
N,N,2-TRIMETHYL-5-NITRO-BENZENESULFONAMIDE
Benzenesulfonamide, N,N,2-trimethyl-5-nitro-
3-(N,N-Dimethylsulfonamido)-4-methylnitrobenzene,5-Nitro-2-N,N-trimethylbenzenesulfonamide | [EINECS(EC#)]
1592732-453-0 | [Molecular Formula]
C9H12N2O4S | [MDL Number]
MFCD03039912 | [MOL File]
433695-36-4.mol | [Molecular Weight]
244.27 |
| Chemical Properties | Back Directory | [Appearance]
Off-White Solid | [Melting point ]
65-67°C | [Boiling point ]
391.1±52.0 °C(Predicted) | [density ]
1.334±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C
| [solubility ]
DMSO: 12 mg/mL
| [form ]
solid
| [pka]
-5?+-.0.70(Predicted) | [color ]
white
| [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. |
| Hazard Information | Back Directory | [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). | [storage]
Store at +4°C | [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 |
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