| 产品描述: | 选择性PDE7抑制剂;Selective PDE7 inhibitor;BRL-50481 is a selective inhibitor of phosphodiesterase 7 (PDE 7) that has acceptable selectivity for in vitro studies. Studies suggest that BRL-50481 is used to inhibit the activity of hrPDE7A1 which is usually expressed in baculovirus-infected Spodoptera frugiperda in a competitive manner. In osteoblasts, BRL-50481increases mineralization and bALP as a result of PDE7 silencing which upregulates several osteogenic genes. Further studies show that BRL-50481increases apoptosis in CLL cells via a mitochondrial-dependent process, and is associated with increased cAMP accumulation and down-regulation of the antiapoptotic protein survivin. BRL-50481 is a inhibitor of PDE7A.;BRL-50481 is a selective inhibitor of phosphodiesterase 7 (PDE 7) that has acceptable selectivity for in vitro studies. Studies suggest that BRL-50481 is used to inhibit the activity of hrPDE7A1 which is usually expressed in baculovirus-infected Spodoptera frugiperda in a competitive manner. In osteoblasts, BRL-50481increases mineralization and bALP as a result of PDE7 silencing which upregulates several osteogenic genes. Further studies show that BRL-50481increases apoptosis in CLL cells via a mitochondrial-dependent process, and is associated with increased cAMP accumulation and down-regulation of the antiapoptotic protein survivin. BRL-50481 is a inhibitor of PDE7A. |
| 参考文献: |
1. Safavi M, et al. New methods for the discovery and synthesis of PDE7 inhibitors as new drugs for neurologicaland inflammatory disorders. Expert Opin Drug Discov. 2013 Jun;8(6):733-51. 2. Smith SJ, et al. 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. 2004 Dec;66(6):1679-89. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
4.094 ml |
20.469 ml |
40.938 ml |
| 5 mM |
0.819 ml |
4.094 ml |
8.188 ml |
| 10 mM |
0.409 ml |
2.047 ml |
4.094 ml |
| 50 mM |
0.082 ml |
0.409 ml |
0.819 ml |
|
| 注意: |
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