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| BRL 50481 Basic information |
| Product Name: | BRL 50481 | | Synonyms: | 5-NITRO-2,N,N-TRIMETHYLBENZENESULFONAMIDE;BRL 50481;N,N,2-TRIMETHYL-5-NITRO-BENZENESULFONAMIDE;3-(N,N-Dimethylsulfonamido)-4-methylnitrobenzene,5-Nitro-2-N,N-trimethylbenzenesulfonamide;Benzenesulfonamide, N,N,2-trimethyl-5-nitro-;-50481 | | CAS: | 433695-36-4 | | MF: | C9H12N2O4S | | MW: | 244.27 | | EINECS: | 1592732-453-0 | | Product Categories: | All Inhibitors;Inhibitors;Cyclic Nucleotide related | | Mol File: | 433695-36-4.mol |
| BRL 50481 Chemical Properties |
| 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. |
| BRL 50481 Usage And Synthesis |
| 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. | | 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. | | 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 |
| BRL 50481 Preparation Products And Raw materials |
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