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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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N423955-1ml | 1ml | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $241.90 |
Selective PDE7 inhibitor
Synonyms | 433695-36-4 | BRL-50481 | BRL 50481 | N,N,2-trimethyl-5-nitrobenzenesulfonamide | 5-Nitro-2,N,N-trimethylbenzenesulfonamide | N,N,2-Trimethyl-5-nitro-benzenesulfonamide | Benzenesulfonamide, N,N,2-trimethyl-5-nitro- | BRL50481 | CHEMBL484928 | N,N,2-trimethyl-5-nitrobenzen |
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Specifications & Purity | Moligand™, 10mM in DMSO |
Biochemical and Physiological Mechanisms | BRL 50481 is a potent and selective PDE7 inhibitor (IC50 = 260 nM).Selective, competitive PDE7 inhibitor (IC 50 values are 0.15 and 12.1 μm for PDE7A and PDE7B respectively). Active in vivo and in vitro . Potentiates the anti-inflammatory effect of PDE4 i |
Storage Temp | Store at -80°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Product Description | 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. |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | N,N,2-trimethyl-5-nitrobenzenesulfonamide |
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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 |
InChi Key | IFIUFCJFLGCQPH-UHFFFAOYSA-N |
Canonical SMILES | CC1=C(C=C(C=C1)[N+](=O)[O-])S(=O)(=O)N(C)C |
Isomeric SMILES | CC1=C(C=C(C=C1)[N+](=O)[O-])S(=O)(=O)N(C)C |
WGK Germany | 3 |
PubChem CID | 2921148 |
Molecular Weight | 244.27 |
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Sensitivity | Heat Sensitive |
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Melt Point(°C) | 73 °C |
WGK Germany | 3 |
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